Talazoparib 100microgram capsules
Prescription only
Requires a prescription from a doctor or prescriber
Capsule
Oral
Cytotoxic drugs
Active ingredients:
Talazoparib
No active safety alerts
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Safety monitoring data
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The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Talazoparib
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Talazoparib
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Talzenna 0.1mg capsules
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Talazoparib 1mg capsules
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Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Talazoparib
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(4)
Talazoparib with enzalutamide for untreated hormone-relapsed metastatic prostate cancer (TA1130)
TA1130
Technology appraisal
Updated Feb 2026Talazoparib for treating HER2-negative advanced breast cancer with germline BRCA mutations (TA952)
TA952
Technology appraisal
Updated Feb 2024Olaparib for treating BRCA mutation-positive HER2-negative advanced breast cancer after chemotherapy (TA1040)
TA1040
Technology appraisal
Updated Feb 2025Early and locally advanced breast cancer: diagnosis and management (NG101)
NG101
NICE guideline
Updated Apr 2025Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
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Codes for healthcare professionals and prescribing systems
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
Not available
Mechanism
Poly(ADP-ribose) polymerases (PARPs) are multifunctional enzymes involved in ess…
Food interactions
2 warnings
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1 mg
After administration of talazoparib 1 mg orally once daily, the mean [% coefficient of variation (CV%)] AUC and maximum observed plasma concentration…
Half-life
The mean terminal plasma half-life (±standard deviation) is 90 (±58) hours in patients with cancer.
[A260346][L47236]
[A260346][L47236]
Protein binding
74%
In vitro, the protein binding of talazoparib is 74% and is independent of talazoparib concentration.
[L47236]
[L47236]
Volume of distribution
420 L
The mean apparent volume of distribution of talazoparib is 420 L.
[L47236]
[L47236]
Metabolism
Talazoparib undergoes minimal hepatic metabolism. The metabolic pathways include mono-oxidation, dehydrogenation, cysteine conjugation of mono-desfluoro talazoparib, and glucuronide conjugation.
[L47236]…
[L47236]…
Elimination
68.7%
The major route of elimination is renal excretion. Approximately 68.7%…
Clearance
6.45 L/h
The mean apparent oral clearance is 6.45 L/h. The inter-subject variability is 31%.
[L47236]
[L47236]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Talazoparib is an inhibitor of mammalian polyadenosine 5’-diphosphoribose polymerases (PARPs), enzymes responsible for regulating essential cellular functions, such as DNA transcription and DNA repair.[L47236]
Developed by Pfizer, talazoparib was first approved by the FDA in October 2018 [A260346] and by the EMA in June 2019.[L47296] It was approved by Health Canada in September 2020.[L47301] Talazoparib is currently used in the treatment of BRCA-mutated breast cancer and HRR-mutated prostate cancer.[L47236][L47301][L47306]
Developed by Pfizer, talazoparib was first approved by the FDA in October 2018 [A260346] and by the EMA in June 2019.[L47296] It was approved by Health Canada in September 2020.[L47301] Talazoparib is currently used in the treatment of BRCA-mutated breast cancer and HRR-mutated prostate cancer.[L47236][L47301][L47306]
Properties:
solid
Avg. mass: 380.36 Da
DrugBank indication
Talazoparib is indicated for the treatment of adult patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) HER2-negative locally advanced or metastatic breast cancer. This indication is approved by the FDA, EMA, and Health Canada.
[L47236][L47301][L47306]
Talazoparib is also indicated in combination with [enzalutamide] for the treatment of adult patients with HRR gene-mutated metastatic castration-resistant prostate cancer (mCRPC).
[L47236][L47306]
[L47236][L47301][L47306]
Talazoparib is also indicated in combination with [enzalutamide] for the treatment of adult patients with HRR gene-mutated metastatic castration-resistant prostate cancer (mCRPC).
[L47236][L47306]
Also known as(42)
Talazoparib
2.4.2.30
ADP-ribosyltransferase diphtheria toxin-like 1
ADPRT
ADPRT 1
ARTD1
DNA ADP-ribosyltransferase PARP1
NAD(+) ADP-ribosyltransferase 1
Dosage forms(21)
(Oral) — 0.1 mg
(Oral) — 0.25 mg
(Oral) — 1 mg
Capsule (Oral) — 0.1 mg/1
Capsule (Oral) — 0.1 mg
Capsule (Oral) — 0.25 mg/1
Capsule (Oral) — 0.35 mg
Capsule (Oral) — 0.35 mg/1
Molecular properties(19)
Drug interactions(348)
Known interactions with other medications. Always consult a healthcare professional.
Ranolazine
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Ranolazine.
Lumacaftor
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Lumacaftor.
Vemurafenib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Vemurafenib.
Apalutamide
Unknown severity
The serum concentration of Talazoparib can be decreased when it is combined with Apalutamide.
Pitolisant
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Pitolisant.
Isavuconazole
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Isavuconazole.
Isavuconazonium
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Isavuconazonium.
Pravastatin
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Pravastatin.
Diethylstilbestrol
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Diethylstilbestrol.
The serum concentration of Talazoparib can be increased when it is combined with Estradiol.
Sulfasalazine
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Sulfasalazine.
Novobiocin
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Novobiocin.
Hesperetin
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Hesperetin.
Rabeprazole
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Rabeprazole.
Dexamethasone
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Dexamethasone.
The serum concentration of Talazoparib can be increased when it is combined with Dasatinib.
Topiroxostat
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Topiroxostat.
The serum concentration of Talazoparib can be increased when it is combined with Daidzin.
Fusidic acid
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Fusidic acid.
Naringenin
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Naringenin.
Eltrombopag
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Eltrombopag.
Safinamide
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Safinamide.
Vismodegib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Vismodegib.
Teriflunomide
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Teriflunomide.
Dabrafenib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Dabrafenib.
Cannabidiol
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Cannabidiol.
The serum concentration of Talazoparib can be increased when it is combined with Dasabuvir.
Fostamatinib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Fostamatinib.
Gilteritinib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Gilteritinib.
Brigatinib
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Brigatinib.
Estradiol acetate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Estradiol acetate.
Estradiol benzoate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Estradiol benzoate.
Estradiol cypionate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Estradiol cypionate.
Estradiol dienanthate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Estradiol dienanthate.
Estradiol valerate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Estradiol valerate.
Nabiximols
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Nabiximols.
The serum concentration of Talazoparib can be increased when it is combined with Caffeine.
Pantoprazole
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Pantoprazole.
Nelfinavir
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Nelfinavir.
The serum concentration of Talazoparib can be increased when it is combined with Gefitinib.
Beclomethasone dipropionate
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Beclomethasone dipropionate.
Progesterone
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Progesterone.
Lansoprazole
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Lansoprazole.
The serum concentration of Talazoparib can be increased when it is combined with Imatinib.
Buprenorphine
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Buprenorphine.
Telmisartan
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Telmisartan.
The serum concentration of Talazoparib can be increased when it is combined with Sunitinib.
The serum concentration of Talazoparib can be increased when it is combined with Genistein.
The serum concentration of Talazoparib can be increased when it is combined with Quercetin.
Rilpivirine
Unknown severity
The serum concentration of Talazoparib can be increased when it is combined with Rilpivirine.
Showing 50 of 348 interactions
Food & lifestyle interactions
Advice
Take at the same time every day.
Advice
Take with or without food. A high-fat, high-calorie meal decreases Cmax and delays Tmax, but not to a clinically significant extent.
Toxicity & overdose
There is no information available regarding the acute toxicity (LD50) of talazoparib. There is no specific treatment in the event of talazoparib overdose, and symptoms of overdose have not been established. In the event of an overdose, discontinue treatment with talazoparib, consider gastric decontamination, follow general supportive measures, and treat symptomatically.
[L47236]
[L47236]
How it works
Mechanism of action
Poly(ADP-ribose) polymerases (PARPs) are multifunctional enzymes involved in essential cellular functions, such as DNA transcription and DNA repair. PARPs recognize and repair DNA single-strand breaks (SSBs) via the base excision repair (BER) pathway. DNA double-strand breaks (DSBs) are repaired via homologous recombination by tumour suppressor proteins encoded by BRCA1 and BRCA2.[A245985][A260346]
Talazoparib is a potent inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1 and PARP2.[L47236] In vitro, talazoparib binds to PARP-1 and -2 isoforms with similar affinity.[A260346] Inhibition of the BER pathway by talazoparib leads to the accumulation of unrepaired SSBs, which leads to the formation of DSBs, which is the most toxic form of DNA damage. While BRCA-dependent homologous recombination can repair DSBs in normal cells, this repair pathway is defective in cells with BRCA1/2 mutations, such as certain tumour cells.[A246015] Inhibition of PARP in cancer cells with BRCA mutations leads to genomic instability and apoptotic cell death. This end result is also referred to as synthetic lethality, a phenomenon where the combination of two defects - inhibition of PARP activity and loss of DSB repair by HR - that are otherwise benign when alone leads to detrimental results.[A39537][A245985] By inhibiting PARP, talazoparib increases the formation of PARP-DNA complexes resulting in DNA damage, decreased cell proliferation, and apoptosis.[L47236]
Talazoparib is a potent inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1 and PARP2.[L47236] In vitro, talazoparib binds to PARP-1 and -2 isoforms with similar affinity.[A260346] Inhibition of the BER pathway by talazoparib leads to the accumulation of unrepaired SSBs, which leads to the formation of DSBs, which is the most toxic form of DNA damage. While BRCA-dependent homologous recombination can repair DSBs in normal cells, this repair pathway is defective in cells with BRCA1/2 mutations, such as certain tumour cells.[A246015] Inhibition of PARP in cancer cells with BRCA mutations leads to genomic instability and apoptotic cell death. This end result is also referred to as synthetic lethality, a phenomenon where the combination of two defects - inhibition of PARP activity and loss of DSB repair by HR - that are otherwise benign when alone leads to detrimental results.[A39537][A245985] By inhibiting PARP, talazoparib increases the formation of PARP-DNA complexes resulting in DNA damage, decreased cell proliferation, and apoptosis.[L47236]
Pharmacodynamics
Talazoparib is a cytotoxic and anti-tumour agent. In vitro, talazoparib caused cytotoxicity in cancer cell lines that harboured defects in DNA repair genes, including BRCA1 and BRCA2. Talazoparib mediated anti-tumour effects on patient-derived xenograft breast cancer models bearing mutated BRCA1 or mutated BRCA2 or wild type BRCA1 and BRCA2.[A260346][L47236]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
After administration of talazoparib 1 mg orally once daily, the mean [% coefficient of variation (CV%)] AUC and maximum observed plasma concentration (Cmax) of talazoparib at steady-state was 208 (37%) ng x hr/mL and 16.4 (32%) ng/mL, respectively. The mean (CV%) steady-state Ctrough was 3.53 (61%) ng/mL.
[L47236]
Steady state was reached within two to three weeks of therapy.
[A260346]
The Tmax ranges from one to two hours.
[L47236]
A high-fat, high-calorie food increased the mean Cmax by 46% and the median Tmax from one to four hours, without affecting the AUC.
[L47236]
[L47236]
Steady state was reached within two to three weeks of therapy.
[A260346]
The Tmax ranges from one to two hours.
[L47236]
A high-fat, high-calorie food increased the mean Cmax by 46% and the median Tmax from one to four hours, without affecting the AUC.
[L47236]
Half-life
The mean terminal plasma half-life (±standard deviation) is 90 (±58) hours in patients with cancer.
[A260346][L47236]
[A260346][L47236]
Protein binding
In vitro, the protein binding of talazoparib is 74% and is independent of talazoparib concentration.
[L47236]
[L47236]
Volume of distribution
The mean apparent volume of distribution of talazoparib is 420 L.
[L47236]
[L47236]
Metabolism
Talazoparib undergoes minimal hepatic metabolism. The metabolic pathways include mono-oxidation, dehydrogenation, cysteine conjugation of mono-desfluoro talazoparib, and glucuronide conjugation.
[L47236]
[L47236]
Route of elimination
The major route of elimination is renal excretion. Approximately 68.7% of the total administered radiolabeled dose of talazoparib was recovered in urine, where 54.6% of that dose was in the form of an unchanged drug. About 19.7% of the drug was recovered in feces, with 13.6% of the dose is unchanged.
[L47236]
[L47236]
Clearance
The mean apparent oral clearance is 6.45 L/h. The inter-subject variability is 31%.
[L47236]
[L47236]
Drug targets(2)
Proteins and enzymes this drug interacts with in the body
Poly [ADP-ribose] polymerase 1
PARP1
inhibitor
Specific functionchromatin binding
Cellular location
Chromosome
General function & pharmacology
Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair .
PMID:17177976 PMID:18055453 PMID:18172500 PMID:19344625 PMID:19661379 PMID:20388712 PMID:21680843 PMID:22582261 PMID:23230272 PMID:25043379 PMID:26344098 PMID:26626479 PMID:26626480 PMID:30104678 PMID:31796734 PMID:32028527 PMID:32241924 PMID:32358582 PMID:33186521 PMID:34465625 PMID:34737271
Mediates glutamate, aspartate, serine, histidine or tyrosine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units .
PMID:19764761 PMID:25043379 PMID:28190768 PMID:29954836 PMID:35393539 PMID:7852410 PMID:9315851
Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage .
PMID:33186521 PMID:34874266
Specificity for the different amino acids is conferred by interacting factors, such as HPF1 and NMNAT1 .
PMID:28190768 PMID:29954836 PMID:32028527 PMID:33186521 PMID:33589610 PMID:34625544 PMID:34874266
Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 confers serine specificity by completing the PARP1 active site .
PMID:28190768 PMID:29954836 PMID:32028527 PMID:33186521 PMID:33589610 PMID:34625544 PMID:34874266
Also catalyzes tyrosine ADP-ribosylation of target proteins following interaction with HPF1 .
PMID:29954836 PMID:30257210
Following interaction with NMNAT1, catalyzes glutamate and aspartate ADP-ribosylation of target proteins; NMNAT1 confers glutamate and aspartate specificity (By similarity). PARP1 initiates the repair of DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones (H2BS6ADPr and H3S10ADPr), thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks .
PMID:17177976 PMID:18172500 PMID:19344625 PMID:19661379 PMID:23230272 PMID:27067600 PMID:34465625 PMID:34874266
HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP1 in order to limit the length of poly-ADP-ribose chains .
PMID:33683197 PMID:34732825 PMID:34795260
In addition to base excision repair (BER) pathway, also involved in double-strand breaks (DSBs) repair: together with TIMELESS, accumulates at DNA damage sites and promotes homologous recombination repair by mediating poly-ADP-ribosylation .
PMID:26344098 PMID:30356214
Mediates the poly-ADP-ribosylation of a number of proteins, including itself, APLF, CHFR, RPA1 and NFAT5 .
PMID:17396150 PMID:19764761 PMID:24906880 PMID:34049076
In addition to proteins, also able to ADP-ribosylate DNA: catalyzes ADP-ribosylation of DNA strand break termini containing terminal phosphates and a 2'-OH group in single- and double-stranded DNA, respectively .
PMID:27471034
Required for PARP9 and DTX3L recruitment to DNA damage sites .
PMID:23230272
PARP1-dependent PARP9-DTX3L-mediated ubiquitination promotes the rapid and specific recruitment of 53BP1/TP53BP1, UIMC1/RAP80, and BRCA1 to DNA damage sites .
PMID:23230272
PARP1-mediated DNA repair in neurons plays a role in sleep: senses DNA damage in neurons and promotes sleep, facilitating efficient DNA repair (By similarity). In addition to DNA repair, also involved in other processes, such as transcription regulation, programmed cell death, membrane repair, adipogenesis and innate immunity .
PMID:15607977 PMID:17177976 PMID:19344625 PMID:27256882 PMID:32315358 PMID:32844745 PMID:35124853 PMID:35393539 PMID:35460603
Acts as a repressor of transcription: binds to nucleosomes and modulates chromatin structure in a manner similar to histone H1, thereby altering RNA polymerase II .
PMID:15607977 PMID:22464733
Acts both as a positive and negative regulator of transcription elongation, depending on the context .
PMID:27256882 PMID:35393539
Acts as a positive regulator of transcription elongation by mediating poly-ADP-ribosylation of NELFE, preventing RNA-binding activity of NELFE and relieving transcription pausing .
PMID:27256882
Acts as a negative regulator of transcription elongation in response to DNA damage by catalyzing poly-ADP-ribosylation of CCNT1, disrupting the phase separation activity of CCNT1 and subsequent activation of CDK9 .
PMID:35393539
Involved in replication fork progression following interaction with CARM1: mediates poly-ADP-ribosylation at replication forks, slowing fork progression .
PMID:33412112
Poly-ADP-ribose chains generated by PARP1 also play a role in poly-ADP-ribose-dependent cell death, a process named parthanatos (By similarity).
Also acts as a negative regulator of the cGAS-STING pathway .
PMID:32315358 PMID:32844745 PMID:35460603
Acts by mediating poly-ADP-ribosylation of CGAS: PARP1 translocates into the cytosol following phosphorylation by PRKDC and catalyzes poly-ADP-ribosylation and inactivation of CGAS .
PMID:35460603
Acts as a negative regulator of adipogenesis: catalyzes poly-ADP-ribosylation of histone H2B on 'Glu-35' (H2BE35ADPr) following interaction with NMNAT1, inhibiting phosphorylation of H2B at 'Ser-36' (H2BS36ph), thereby blocking expression of pro-adipogenetic genes (By similarity). Involved in the synthesis of ATP in the nucleus, together with NMNAT1, PARG and NUDT5 .
PMID:27257257
Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming PMID:27257257
PMID:17177976 PMID:18055453 PMID:18172500 PMID:19344625 PMID:19661379 PMID:20388712 PMID:21680843 PMID:22582261 PMID:23230272 PMID:25043379 PMID:26344098 PMID:26626479 PMID:26626480 PMID:30104678 PMID:31796734 PMID:32028527 PMID:32241924 PMID:32358582 PMID:33186521 PMID:34465625 PMID:34737271
Mediates glutamate, aspartate, serine, histidine or tyrosine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units .
PMID:19764761 PMID:25043379 PMID:28190768 PMID:29954836 PMID:35393539 PMID:7852410 PMID:9315851
Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage .
PMID:33186521 PMID:34874266
Specificity for the different amino acids is conferred by interacting factors, such as HPF1 and NMNAT1 .
PMID:28190768 PMID:29954836 PMID:32028527 PMID:33186521 PMID:33589610 PMID:34625544 PMID:34874266
Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 confers serine specificity by completing the PARP1 active site .
PMID:28190768 PMID:29954836 PMID:32028527 PMID:33186521 PMID:33589610 PMID:34625544 PMID:34874266
Also catalyzes tyrosine ADP-ribosylation of target proteins following interaction with HPF1 .
PMID:29954836 PMID:30257210
Following interaction with NMNAT1, catalyzes glutamate and aspartate ADP-ribosylation of target proteins; NMNAT1 confers glutamate and aspartate specificity (By similarity). PARP1 initiates the repair of DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones (H2BS6ADPr and H3S10ADPr), thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks .
PMID:17177976 PMID:18172500 PMID:19344625 PMID:19661379 PMID:23230272 PMID:27067600 PMID:34465625 PMID:34874266
HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP1 in order to limit the length of poly-ADP-ribose chains .
PMID:33683197 PMID:34732825 PMID:34795260
In addition to base excision repair (BER) pathway, also involved in double-strand breaks (DSBs) repair: together with TIMELESS, accumulates at DNA damage sites and promotes homologous recombination repair by mediating poly-ADP-ribosylation .
PMID:26344098 PMID:30356214
Mediates the poly-ADP-ribosylation of a number of proteins, including itself, APLF, CHFR, RPA1 and NFAT5 .
PMID:17396150 PMID:19764761 PMID:24906880 PMID:34049076
In addition to proteins, also able to ADP-ribosylate DNA: catalyzes ADP-ribosylation of DNA strand break termini containing terminal phosphates and a 2'-OH group in single- and double-stranded DNA, respectively .
PMID:27471034
Required for PARP9 and DTX3L recruitment to DNA damage sites .
PMID:23230272
PARP1-dependent PARP9-DTX3L-mediated ubiquitination promotes the rapid and specific recruitment of 53BP1/TP53BP1, UIMC1/RAP80, and BRCA1 to DNA damage sites .
PMID:23230272
PARP1-mediated DNA repair in neurons plays a role in sleep: senses DNA damage in neurons and promotes sleep, facilitating efficient DNA repair (By similarity). In addition to DNA repair, also involved in other processes, such as transcription regulation, programmed cell death, membrane repair, adipogenesis and innate immunity .
PMID:15607977 PMID:17177976 PMID:19344625 PMID:27256882 PMID:32315358 PMID:32844745 PMID:35124853 PMID:35393539 PMID:35460603
Acts as a repressor of transcription: binds to nucleosomes and modulates chromatin structure in a manner similar to histone H1, thereby altering RNA polymerase II .
PMID:15607977 PMID:22464733
Acts both as a positive and negative regulator of transcription elongation, depending on the context .
PMID:27256882 PMID:35393539
Acts as a positive regulator of transcription elongation by mediating poly-ADP-ribosylation of NELFE, preventing RNA-binding activity of NELFE and relieving transcription pausing .
PMID:27256882
Acts as a negative regulator of transcription elongation in response to DNA damage by catalyzing poly-ADP-ribosylation of CCNT1, disrupting the phase separation activity of CCNT1 and subsequent activation of CDK9 .
PMID:35393539
Involved in replication fork progression following interaction with CARM1: mediates poly-ADP-ribosylation at replication forks, slowing fork progression .
PMID:33412112
Poly-ADP-ribose chains generated by PARP1 also play a role in poly-ADP-ribose-dependent cell death, a process named parthanatos (By similarity).
Also acts as a negative regulator of the cGAS-STING pathway .
PMID:32315358 PMID:32844745 PMID:35460603
Acts by mediating poly-ADP-ribosylation of CGAS: PARP1 translocates into the cytosol following phosphorylation by PRKDC and catalyzes poly-ADP-ribosylation and inactivation of CGAS .
PMID:35460603
Acts as a negative regulator of adipogenesis: catalyzes poly-ADP-ribosylation of histone H2B on 'Glu-35' (H2BE35ADPr) following interaction with NMNAT1, inhibiting phosphorylation of H2B at 'Ser-36' (H2BS36ph), thereby blocking expression of pro-adipogenetic genes (By similarity). Involved in the synthesis of ATP in the nucleus, together with NMNAT1, PARG and NUDT5 .
PMID:27257257
Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming PMID:27257257
Poly [ADP-ribose] polymerase 2
PARP2
inhibitor
Specific functionchromatin binding
Cellular location
Nucleus
General function & pharmacology
Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair .
PMID:10364231 PMID:25043379 PMID:27471034 PMID:30104678 PMID:32028527 PMID:32939087 PMID:34108479 PMID:34486521 PMID:34874266
Mediates glutamate, aspartate or serine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units .
PMID:25043379 PMID:30104678 PMID:30321391
Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage .
PMID:32939087
Mediates glutamate and aspartate ADP-ribosylation of target proteins in absence of HPF1 .
PMID:25043379
Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 conferring serine specificity by completing the PARP2 active site .
PMID:28190768 PMID:32028527 PMID:34108479 PMID:34486521 PMID:34874266
PARP2 initiates the repair of double-strand DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones, thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks .
PMID:10364231 PMID:32939087 PMID:34108479
HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP2 in order to limit the length of poly-ADP-ribose chains .
PMID:34732825 PMID:34795260
Specifically mediates formation of branched poly-ADP-ribosylation .
PMID:30104678
Branched poly-ADP-ribose chains are specifically recognized by some factors, such as APLF .
PMID:30104678
In addition to proteins, also able to ADP-ribosylate DNA: preferentially acts on 5'-terminal phosphates at DNA strand breaks termini in nicked duplex PMID:27471034 PMID:29361132
PMID:10364231 PMID:25043379 PMID:27471034 PMID:30104678 PMID:32028527 PMID:32939087 PMID:34108479 PMID:34486521 PMID:34874266
Mediates glutamate, aspartate or serine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units .
PMID:25043379 PMID:30104678 PMID:30321391
Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage .
PMID:32939087
Mediates glutamate and aspartate ADP-ribosylation of target proteins in absence of HPF1 .
PMID:25043379
Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 conferring serine specificity by completing the PARP2 active site .
PMID:28190768 PMID:32028527 PMID:34108479 PMID:34486521 PMID:34874266
PARP2 initiates the repair of double-strand DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones, thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks .
PMID:10364231 PMID:32939087 PMID:34108479
HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP2 in order to limit the length of poly-ADP-ribose chains .
PMID:34732825 PMID:34795260
Specifically mediates formation of branched poly-ADP-ribosylation .
PMID:30104678
Branched poly-ADP-ribose chains are specifically recognized by some factors, such as APLF .
PMID:30104678
In addition to proteins, also able to ADP-ribosylate DNA: preferentially acts on 5'-terminal phosphates at DNA strand breaks termini in nicked duplex PMID:27471034 PMID:29361132
Transporters(2)
Proteins that transport this drug across cell membranes
ATP-dependent translocase ABCB1
ABCB1
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
Scientific references(3)
Javle M., Curtin N.J.
The role of PARP in DNA repair and its therapeutic exploitation.
British Journal Cancer
2011 Oct 11105(8):1114-22. doi: 10.1038/bjc.2011.382
Hoy S.M.
Talazoparib: First Global Approval.
Drugs
2018 Dec78(18):1939-1946. doi: 10.1007/s40265-018-1026-z
Bochum S., Berger S., Martens U.M.
Olaparib.
Recent Results Cancer Research
2018211:217-233. doi: 10.1007/978-3-319-91442-8_15
ATC classification(1 code)
ATC L01XK04
Salt forms(1)
Talazoparib tosylate(DBSALT002816)
Commercial products(28)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Talazoparib
Additional database identifiers
Drugs Product Database (DPD)
23356
ChemSpider
28637772
BindingDB
50084621
PDB
2YQ
ZINC
ZINC000072318110
HUGO Gene Nomenclature Committee (HGNC)
HGNC:270
GenAtlas
PARP1
GeneCards
PARP1
GenBank Gene Database
X16674
GenBank Protein Database
1017423
Guide to Pharmacology
2771
UniProt Accession
PARP1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:272
GeneCards
PARP2
GenBank Gene Database
AJ236912
GenBank Protein Database
6688130
Guide to Pharmacology
2772
UniProt Accession
PARP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
Patent information
6 active patents
8735392
United States
Approved 27 May 2014 · Expires 20 Oct 2031
5y 6m
10189837
United States
Approved 29 Jan 2019 · Expires 20 Oct 2031
5y 6m
8012976
United States
Approved 6 Sept 2011 · Expires 19 Oct 2029
3y 6m
9820985
United States
Approved 21 Nov 2017 · Expires 27 Jul 2029
3y 3m
8420650
United States
Approved 16 Apr 2013 · Expires 27 Jul 2029
3y 3m
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated about 1 month ago(4 Mar 2026)