Mobocertinib 40mg capsules
Capsule
40mg
Oral
Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR).
Active ingredients:
Mobocertinib
No active safety alerts
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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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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.
Clinical guidelines and formulary information
British National Formulary
Mobocertinib
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.
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Supply & product information
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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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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
18 hours
Mechanism
The epidermal growth factor receptor (EGFR) is a transmembrane receptor that reg…
Food interactions
2 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
37%
The mean absolute bioavailability of mobocertinib is 37% and the median Tmax is approximately 4 hours.
[L38319]…
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Half-life
18 hours
At steady-state, the mean elimination half-life of mobocertinib and its two active metabolites, AP32960 and AP32914, was 18 hours, 24 hours, and 18 hours, respectively.
[L38319]…
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Protein binding
99.3%
Mobocertinib and its metabolites are extensively protein-bound in plasma, although the specific proteins to which they bind have not been elucidated.…
Volume of distribution
509 L
The mean apparent volume of distribution of mobocertinib was approximately 3,509 L at steady-state.
[L38319]
[L38319]
Metabolism
36%
Mobocertinib is metabolized primarily by CYP3A enzymes to two active metabolites, AP32960 and AP32914, which are equipotent to mobocertinib and…
Elimination
76%
Following oral administration of mobocertinib, approximately 76% of the administered dose was recovered in the feces (6% as unchanged parent…
Clearance
138 L/h
At steady-state, the mean apparent oral clearance of mobocertinib and its two active metabolites, AP32960 and AP32914, was 138 L/hr, 149 L/hr, and 159 L/hr, respectively.
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Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Withdrawn
Small molecule
About this compound
Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used specifically in the treatment of non-small cell lung cancer (NSCLC) caused by exon 20 insertion mutations in the EGFR gene,[L38368] which are typically associated with a poorer prognosis (as compared to "classical" EGFR mutants causing NSCLC) and are associated with resistance to standard targeted EGFR inhibitors.[A238828] Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.[L38319]
Mobocertinib, under the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated approval by the FDA in September 2021 for the treatment of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.[L38368]
Mobocertinib, under the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated approval by the FDA in September 2021 for the treatment of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.[L38368]
Properties:
solid
Avg. mass: 585.71 Da
DrugBank indication
Mobocertinib is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy.
[L38319]
[L38319]
Also known as(46)
Mobocertinib
2.7.10.1
ERBB
ERBB1
HER1
Proto-oncogene c-ErbB-1
Receptor tyrosine-protein kinase erbB-1
1,4-cineole 2-exo-monooxygenase
Dosage forms(1)
Capsule (Oral) — 40 mg/1
Molecular properties(19)
Drug interactions(777)
Known interactions with other medications. Always consult a healthcare professional.
Leuprolide
Unknown severity
The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Goserelin is combined with Mobocertinib.
Octreotide
Unknown severity
The risk or severity of QTc prolongation can be increased when Octreotide is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Oxytocin is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Esmolol is combined with Mobocertinib.
Bortezomib
Unknown severity
The risk or severity of QTc prolongation can be increased when Bortezomib is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Betaxolol is combined with Mobocertinib.
Fluconazole
Unknown severity
The risk or severity of QTc prolongation can be increased when Fluconazole is combined with Mobocertinib.
Erythromycin
Unknown severity
The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Mobocertinib.
Dofetilide
Unknown severity
The risk or severity of QTc prolongation can be increased when Dofetilide is combined with Mobocertinib.
Azithromycin
Unknown severity
The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Mobocertinib.
Citalopram
Unknown severity
The risk or severity of QTc prolongation can be increased when Citalopram is combined with Mobocertinib.
Moxifloxacin
Unknown severity
The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Mobocertinib.
Nelfinavir
Unknown severity
The risk or severity of QTc prolongation can be increased when Nelfinavir is combined with Mobocertinib.
Pregabalin
Unknown severity
The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Mobocertinib.
Ranolazine
Unknown severity
The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Mobocertinib.
Benzatropine
Unknown severity
The risk or severity of QTc prolongation can be increased when Benzatropine is combined with Mobocertinib.
Ziprasidone
Unknown severity
The risk or severity of QTc prolongation can be increased when Ziprasidone is combined with Mobocertinib.
Anagrelide
Unknown severity
The risk or severity of QTc prolongation can be increased when Anagrelide is combined with Mobocertinib.
Sulfisoxazole
Unknown severity
The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Mobocertinib.
Isradipine
Unknown severity
The risk or severity of QTc prolongation can be increased when Isradipine is combined with Mobocertinib.
Disopyramide
Unknown severity
The risk or severity of QTc prolongation can be increased when Disopyramide is combined with Mobocertinib.
Clemastine
Unknown severity
The risk or severity of QTc prolongation can be increased when Clemastine is combined with Mobocertinib.
Atomoxetine
Unknown severity
The risk or severity of QTc prolongation can be increased when Atomoxetine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Ibutilide is combined with Mobocertinib.
Valproic acid
Unknown severity
The risk or severity of QTc prolongation can be increased when Valproic acid is combined with Mobocertinib.
Amitriptyline
Unknown severity
The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Methadone is combined with Mobocertinib.
Olanzapine
Unknown severity
The risk or severity of QTc prolongation can be increased when Olanzapine is combined with Mobocertinib.
Cetirizine
Unknown severity
The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Mobocertinib.
Terfenadine
Unknown severity
The risk or severity of QTc prolongation can be increased when Terfenadine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Mobocertinib.
Protriptyline
Unknown severity
The risk or severity of QTc prolongation can be increased when Protriptyline is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Mobocertinib.
Trimethadione
Unknown severity
The risk or severity of QTc prolongation can be increased when Trimethadione is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Buclizine is combined with Mobocertinib.
Mefloquine
Unknown severity
The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Clozapine is combined with Mobocertinib.
Grepafloxacin
Unknown severity
The risk or severity of QTc prolongation can be increased when Grepafloxacin is combined with Mobocertinib.
Doxylamine
Unknown severity
The risk or severity of QTc prolongation can be increased when Doxylamine is combined with Mobocertinib.
Mirtazapine
Unknown severity
The risk or severity of QTc prolongation can be increased when Mirtazapine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Timolol is combined with Mobocertinib.
Treprostinil
Unknown severity
The risk or severity of QTc prolongation can be increased when Treprostinil is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Digoxin is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Mobocertinib.
Nimodipine
Unknown severity
The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Sorafenib is combined with Mobocertinib.
Dexbrompheniramine
Unknown severity
The risk or severity of QTc prolongation can be increased when Dexbrompheniramine is combined with Mobocertinib.
The risk or severity of QTc prolongation can be increased when Promazine is combined with Mobocertinib.
Hyoscyamine
Unknown severity
The risk or severity of QTc prolongation can be increased when Hyoscyamine is combined with Mobocertinib.
Showing 50 of 777 interactions
Food & lifestyle interactions
Advice
Avoid St. John's Wort. St. John's Wort is a potent CYP3A inducer and may decrease the efficacy of mobocertinib.
Advice
Take with or without food. Co-administration with food does not significantly affect the disposition of mobocertinib.
Toxicity & overdose
No data are available regarding overdosage with mobocertinib. Symptoms of overdosage are likely to be consistent with mobocertinib's adverse effects and may therefore include significant gastrointestinal symptoms, pain, fatigue, and rash.
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How it works
Mechanism of action
The epidermal growth factor receptor (EGFR) is a transmembrane receptor that regulates signaling pathways in the control of cellular proliferation.[A19201] Mutations in these proteins have been associated with certain types of lung cancer, including non-small cell lung cancer (NSCLC). While the majority of EGFR mutations associated with NSCLC involve the EGFR L858R point mutation or exon 19 deletions (referred to as "classical" EGFR mutations), less common EGFR exon 20 insertion mutations carry a particularly poor prognosis and are associated with resistance to standard targeted EGFR inhibitors.[A238828]
Mobocertinib is an inhibitor of EGFR that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild-type EGFR proteins, exerting a pharmacologic effect on mutant variants at concentrations 1.5- to 10-fold lower than on wild-type proteins.[L38319]
Mobocertinib is an inhibitor of EGFR that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild-type EGFR proteins, exerting a pharmacologic effect on mutant variants at concentrations 1.5- to 10-fold lower than on wild-type proteins.[L38319]
Pharmacodynamics
Mobocertinib is an inhibitor of EGFR that preferentially targets exon 20 insertion mutant variants.[L38319] It is available as an oral capsule taken with or without food once daily.
Mobocertinib can cause a concentration-dependent increase in QTc interval which may lead to life-threatening complications such as Torsades de Pointes. Patients with baseline risk factors for QTc prolongation should consider alternative medications or be monitored carefully throughout therapy. The use of concomitant QTc-prolonging medications should be avoided, as should concomitant inhibitors of CYP3A, as these may increase the concentration of mobocertinib and thus the risk of QTc-prolongation.[L38319]
Mobocertinib can cause a concentration-dependent increase in QTc interval which may lead to life-threatening complications such as Torsades de Pointes. Patients with baseline risk factors for QTc prolongation should consider alternative medications or be monitored carefully throughout therapy. The use of concomitant QTc-prolonging medications should be avoided, as should concomitant inhibitors of CYP3A, as these may increase the concentration of mobocertinib and thus the risk of QTc-prolongation.[L38319]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
The mean absolute bioavailability of mobocertinib is 37% and the median Tmax is approximately 4 hours.
[L38319]
Following a single oral dose of 160mg of mobocertinib to fasted patients, the mean Cmax and AUC0-inf were 45.8 ng/mL and 862 ng•h/mL, respectively.
[A238743]
[L38319]
Following a single oral dose of 160mg of mobocertinib to fasted patients, the mean Cmax and AUC0-inf were 45.8 ng/mL and 862 ng•h/mL, respectively.
[A238743]
Half-life
At steady-state, the mean elimination half-life of mobocertinib and its two active metabolites, AP32960 and AP32914, was 18 hours, 24 hours, and 18 hours, respectively.
[L38319]
[L38319]
Protein binding
Mobocertinib and its metabolites are extensively protein-bound in plasma, although the specific proteins to which they bind have not been elucidated. Following oral administration, mobocertinib is 99.3% protein-bound, AP32960 is 99.5% protein-bound, and AP32914 is 98.6% protein-bound.
[L38319]
[L38319]
Volume of distribution
The mean apparent volume of distribution of mobocertinib was approximately 3,509 L at steady-state.
[L38319]
[L38319]
Metabolism
Mobocertinib is metabolized primarily by CYP3A enzymes to two active metabolites, AP32960 and AP32914, which are equipotent to mobocertinib and account for 36% and 4% of its combined molar AUC, respectively.
[L38319]
[L38319]
Route of elimination
Following oral administration of mobocertinib, approximately 76% of the administered dose was recovered in the feces (6% as unchanged parent drug) with only 4% recovered in the urine (1% as unchanged parent drug).
[L38319]
The metabolite AP32960 comprised 12% and 1% of the recovered dose found in the feces and urine, respectively, while the metabolite AP32914 was below the detection limit in both.
[L38319]
The metabolite AP32960 comprised 12% and 1% of the recovered dose found in the feces and urine, respectively, while the metabolite AP32914 was below the detection limit in both.
Clearance
At steady-state, the mean apparent oral clearance of mobocertinib and its two active metabolites, AP32960 and AP32914, was 138 L/hr, 149 L/hr, and 159 L/hr, respectively.
[L38319]
[L38319]
Drug targets(1)
Proteins and enzymes this drug interacts with in the body
Epidermal growth factor receptor
EGFR
inhibitor
Specific functionactin filament binding
Cellular location
Cell membrane
General function & pharmacology
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses .
PMID:10805725 PMID:27153536 PMID:2790960 PMID:35538033
Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF .
PMID:12297049 PMID:15611079 PMID:17909029 PMID:20837704 PMID:27153536 PMID:2790960 PMID:7679104 PMID:8144591 PMID:9419975
Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules .
PMID:27153536
May also activate the NF-kappa-B signaling cascade .
PMID:11116146
Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling .
PMID:11602604
Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin .
PMID:11483589
Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration .
PMID:20462955
Plays a role in enhancing learning and memory performance (By similarity).
Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (By similarity)
PMID:10805725 PMID:27153536 PMID:2790960 PMID:35538033
Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF .
PMID:12297049 PMID:15611079 PMID:17909029 PMID:20837704 PMID:27153536 PMID:2790960 PMID:7679104 PMID:8144591 PMID:9419975
Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules .
PMID:27153536
May also activate the NF-kappa-B signaling cascade .
PMID:11116146
Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling .
PMID:11602604
Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin .
PMID:11483589
Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration .
PMID:20462955
Plays a role in enhancing learning and memory performance (By similarity).
Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (By similarity)
Metabolizing enzymes(3)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP3A4Cytochrome P450 3A4
substrate
CYP3A5Cytochrome P450 3A5
substrate
CYP3A7Cytochrome P450 3A7
substrate
Transporters(2)
Proteins that transport this drug across cell membranes
ATP-dependent translocase ABCB1
ABCB1
substrate
inhibitor
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
inhibitor
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(6)
Zhang S., Jin S., Griffin C., Feng Z., Lin J., Venkatakrishnan K., Gupta N.
Effects of Itraconazole and Rifampin on the Pharmacokinetics of Mobocertinib (TAK-788), an Oral Epidermal Growth Factor Receptor Inhibitor, in Healthy Volunteers.
Clinical Pharmacology Drug Development
2021 Sep10(9):1044-1053. doi: 10.1002/cpdd.967. Epub 2021 Jun 19
Zhang S., Jin S., Griffin C., Feng Z., Lin J., Baratta M., Brake R., Venkatakrishnan K., Gupta N.
Single-Dose Pharmacokinetics and Tolerability of the Oral Epidermal Growth Factor Receptor Inhibitor Mobocertinib (TAK-788) in Healthy Volunteers: Low-Fat Meal Effect and Relative Bioavailability of 2 Capsule Products.
Clinical Pharmacology Drug Development
2021 Sep10(9):1028-1043. doi: 10.1002/cpdd.951. Epub 2021 Jun 12
Vasconcelos PENS, Kobayashi I.S., Kobayashi S.S., Costa D.B.
Preclinical characterization of mobocertinib highlights the putative therapeutic window of this novel EGFR inhibitor to EGFR exon 20 insertion mutations.
JTO Clinical Research Reports
2021 Mar2(3). doi: 10.1016/j.jtocrr.2020.100105. Epub 2020 Oct 6
Gonzalvez F., Vincent S., Baker T.E., Gould A.E., Li S., Wardwell S.D., Nadworny S., Ning Y., Zhang S., Huang W.S., Hu Y., Li F., Greenfield M.T., Zech S.G., Das B., Narasimhan N.I., Clackson T., Dalgarno D., Shakespeare W.C., Fitzgerald M., Chouitar J., Griffin R.J., Liu S., Wong K.K., Zhu X., Rivera V.M.
Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.
Cancer Discov
2021 Jul11(7):1672-1687. doi: 10.1158/2159-8290.CD-20-1683. Epub 2021 Feb 25
Bethune G., Bethune D., Ridgway N., Xu Z.
The role of osimertinib in epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer.
Journal of Thoracic Disease
201911(S3):S448-S452. doi: 10.21037/jtd.2018.11.45
Vyse S., Huang P.H.
Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer.
Signal Transduct Target Therapeutics
2019 Mar 84:5. doi: 10.1038/s41392-019-0038-9. eCollection 2019
ATC classification(1 code)
ATC L01EB10
Affected organisms(1)
Humans and other mammals
International brands(1)
Salt forms(1)
Mobocertinib succinate(DBSALT003192)
Experimental properties(1)
Commercial products(1)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Mobocertinib
Additional database identifiers
ChemSpider
84455481
BindingDB
368374
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3236
GenAtlas
EGFR
GeneCards
EGFR
GenBank Gene Database
X00588
GenBank Protein Database
757924
Guide to Pharmacology
1797
UniProt Accession
EGFR_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2638
GenAtlas
CYP3A5
GeneCards
CYP3A5
GenBank Gene Database
J04813
GenBank Protein Database
181346
Guide to Pharmacology
1338
UniProt Accession
CP3A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2640
GeneCards
CYP3A7
GenBank Gene Database
D00408
GenBank Protein Database
220149
UniProt Accession
CP3A7_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
2 active patents
10227342
United States
Approved 12 Mar 2019 · Expires 13 May 2035
9y 1m
9796712
United States
Approved 24 Oct 2017 · Expires 13 May 2035
9y 1m
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 26 days ago(8 Mar 2026)