Entrectinib 100mg capsules
Requires a prescription from a doctor or prescriber
Official documents, adverse reaction reporting, and safety monitoring
Report a side effect
Submit a Yellow Card report to the MHRA
Official medicine documents
Safety monitoring data
Yellow Card reports
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.
View Drug Analysis Profile
Suspected adverse reactions reported for Entrectinib
Browse all iDAP reports
Interactive Drug Analysis Profiles for all medicines
Report a side effect
Submit a Yellow Card report to the MHRA
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.
EudraVigilance
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
View EudraVigilance report
Suspected adverse reactions reported for Entrectinib
About EudraVigilance
Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
MHRA licensed products
View all licensed products for Entrectinib on the MHRA register
Rozlytrek 100mg capsules
Therapeutically similar medicines
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
Entrectinib
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(5)
Entrectinib for treating ROS1-positive advanced non-small-cell lung cancer (TA643)
Entrectinib for treating NTRK fusion-positive solid tumours in people 12 years and over (terminated appraisal) (TA1118)
Crizotinib for treating ROS1-positive advanced non-small-cell lung cancer (TA1021)
Cabozantinib for previously treated advanced differentiated thyroid cancer unsuitable for or refractory to radioactive iodine (TA928)
Pembrolizumab for previously treated endometrial, biliary, colorectal, gastric or small intestine cancer with high microsatellite instability or mismatch repair deficiency (TA914)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
Pharmacy stock checkers
Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
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
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
20 h
Mechanism
Entrectinib is a tyrosine kinase inhibitor which acts on several receptors.
Food interactions
3 warnings
Human targets
7 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
4-5 h
[L8081]…
Half-life
20 h
[L8081]
The active metabolite, M5, has a half-life of 40 h.
Protein binding
99%
[A183797][L8081]
Volume of distribution
551 L
[L8081]
The active metabolite, M5, has an apparent volume of distribution of 81.1…
Metabolism
76%
[L8081]…
Elimination
83%
[L8081]…
Clearance
19.6 L/h
[L8081]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L8081]
Entrectinib is also indicated in adults and children over 12 years old for the treatment of NTRK gene fusion-positive solid tumors which have metastasized or for which surgical resection is likely to result in severe morbidity and for which has progressed on previous therapies or for which no comparable alternative therapies are available.
FoundationOne®Liquid CDx is the only FDA-approved test for the detection of ROS1 rearrangement(s) in NSCLC for selecting patients for treatment with entrectinib.
[L44518]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 897 interactions
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L8081]
Food does not produce a significant effect on the extent of absorption.
[L8081]
The active metabolite, M5, has a half-life of 40 h.
[A183797][L8081]
[L8081]
The active metabolite, M5, has an apparent volume of distribution of 81.1 L. Entrectinib is known to cross the blood-brain barrier.
[A183797]
[L8081]
M5 has similar pharmacological activity to entrectinib and exists at approximately 40% of the steady state concentration of the parent drug. In rats, six in vivo metabolites have been identified including N-dealkylated, N-oxide, hydroxylated, and glucuronide conjugated metabolites.
[A183191]
[L8081]
Of the dose in the feces, 36% was present as entrectinib and 22% as M5.
[L8081]
Proteins and enzymes this drug interacts with in the body
PMID:1281417 PMID:15488758 PMID:17196528 PMID:1849459 PMID:1850821 PMID:22649032 PMID:27445338 PMID:8325889
Can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 but has no effect on neuron survival (By similarity).
Upon dimeric NGF ligand-binding, undergoes homodimerization, autophosphorylation and activation .
PMID:1281417
Recruits, phosphorylates and/or activates several downstream effectors including SHC1, FRS2, SH2B1, SH2B2 and PLCG1 that regulate distinct overlapping signaling cascades driving cell survival and differentiation. Through SHC1 and FRS2 activates a GRB2-Ras-MAPK cascade that regulates cell differentiation and survival. Through PLCG1 controls NF-Kappa-B activation and the transcription of genes involved in cell survival.
Through SHC1 and SH2B1 controls a Ras-PI3 kinase-AKT1 signaling cascade that is also regulating survival. In absence of ligand and activation, may promote cell death, making the survival of neurons dependent on trophic factors
May activate several downstream signaling pathways related to cell differentiation, proliferation, growth and survival including the PI3 kinase-mTOR signaling pathway. Mediates the phosphorylation of PTPN11, an activator of this pathway. May also phosphorylate and activate the transcription factor STAT3 to control anchorage-independent cell growth.
Mediates the phosphorylation and the activation of VAV3, a guanine nucleotide exchange factor regulating cell morphology. May activate other downstream signaling proteins including AKT1, MAPK1, MAPK3, IRS1 and PLCG2
PMID:15494731 PMID:7574684
Upon ligand-binding, undergoes homodimerization, autophosphorylation and activation .
PMID:15494731
Recruits, phosphorylates and/or activates several downstream effectors including SHC1, FRS2, SH2B1, SH2B2 and PLCG1 that regulate distinct overlapping signaling cascades.
Through SHC1, FRS2, SH2B1, SH2B2 activates the GRB2-Ras-MAPK cascade that regulates for instance neuronal differentiation including neurite outgrowth. Through the same effectors controls the Ras-PI3 kinase-AKT1 signaling cascade that mainly regulates growth and survival. Through PLCG1 and the downstream protein kinase C-regulated pathways controls synaptic plasticity.
Thereby, plays a role in learning and memory by regulating both short term synaptic function and long-term potentiation. PLCG1 also leads to NF-Kappa-B activation and the transcription of genes involved in cell survival. Hence, it is able to suppress anoikis, the apoptosis resulting from loss of cell-matrix interactions.
May also play a role in neutrophin-dependent calcium signaling in glial cells and mediate communication between neurons and glia
PMID:11121404 PMID:11387242 PMID:16317043 PMID:17274988 PMID:30061385 PMID:34646012 PMID:34819673
Also acts as a key thinness protein involved in the resistance to weight gain: in hypothalamic neurons, controls energy expenditure acting as a negative regulator of white adipose tissue lipolysis and sympathetic tone to fine-tune energy homeostasis (By similarity). Following activation by ALKAL2 ligand at the cell surface, transduces an extracellular signal into an intracellular response .
PMID:30061385 PMID:33411331 PMID:34646012 PMID:34819673
In contrast, ALKAL1 is not a potent physiological ligand for ALK .
PMID:34646012
Ligand-binding to the extracellular domain induces tyrosine kinase activation, leading to activation of the mitogen-activated protein kinase (MAPK) pathway .
PMID:34819673
Phosphorylates almost exclusively at the first tyrosine of the Y-x-x-x-Y-Y motif .
PMID:15226403 PMID:16878150
Induces tyrosine phosphorylation of CBL, FRS2, IRS1 and SHC1, as well as of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1 .
PMID:15226403 PMID:16878150
ALK activation may also be regulated by pleiotrophin (PTN) and midkine (MDK) .
PMID:11278720 PMID:11809760 PMID:12107166 PMID:12122009
PTN-binding induces MAPK pathway activation, which is important for the anti-apoptotic signaling of PTN and regulation of cell proliferation .
PMID:11278720 PMID:11809760 PMID:12107166
MDK-binding induces phosphorylation of the ALK target insulin receptor substrate (IRS1), activates mitogen-activated protein kinases (MAPKs) and PI3-kinase, resulting also in cell proliferation induction .
PMID:12122009
Drives NF-kappa-B activation, probably through IRS1 and the activation of the AKT serine/threonine kinase .
PMID:15226403 PMID:16878150
Recruitment of IRS1 to activated ALK and the activation of NF-kappa-B are essential for the autocrine growth and survival signaling of MDK PMID:15226403 PMID:16878150
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
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
ATC L01EX14
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)
Entrectinib
Additional database identifiers
Drugs Product Database (DPD)
23398
ChemSpider
24808589
BindingDB
158154
PDB
YMX
ZINC
ZINC000043204146
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8031
GenAtlas
NTRK1
GeneCards
NTRK1
GenBank Gene Database
M23102
GenBank Protein Database
339918
Guide to Pharmacology
1817
UniProt Accession
NTRK1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8033
GeneCards
NTRK3
Guide to Pharmacology
1819
UniProt Accession
NTRK3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10261
GeneCards
ROS1
Guide to Pharmacology
1840
UniProt Accession
ROS1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8032
GeneCards
NTRK2
GenBank Gene Database
U12140
GenBank Protein Database
530791
Guide to Pharmacology
1818
UniProt Accession
NTRK2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:427
GenAtlas
ALK
GeneCards
ALK
GenBank Gene Database
U62540
GenBank Protein Database
2454168
Guide to Pharmacology
1839
UniProt Accession
ALK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6192
GenAtlas
JAK2
GeneCards
JAK2
GenBank Gene Database
AF058925
Guide to Pharmacology
2048
UniProt Accession
JAK2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:19297
GenAtlas
TNK2
GeneCards
TNK2
GenBank Gene Database
L13738
GenBank Protein Database
8850245
Guide to Pharmacology
2246
UniProt Accession
ACK1_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:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
Patent information
14 active patents
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: