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entrectinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5345	1108743-60-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: entrectinib RXDX-101 NMS-E628 RG 6268 rozlytrek	Entrectinib is an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK). Molecular weight: 560.65 Formula: C31H34F2N6O2 CLOGP: 5.16 LIPINSKI: 2 HAC: 8 HDO: 3 TPSA: 85.52 ALOGS: -4.80 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

entrectinib
RXDX-101
NMS-E628
RG 6268
rozlytrek

Entrectinib is an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK).

Molecular weight: 560.65
Formula: C31H34F2N6O2
CLOGP: 5.16
LIPINSKI: 2
HAC: 8
HDO: 3
TPSA: 85.52
ALOGS: -4.80
ROTB: 7

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.60	g	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Aug. 15, 2019	FDA	GENENTECH INC
June 18, 2019	PMDA	Chugai Pharmaceutical

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Ataxia	68.99	47.96	17	446	15178	63473381
Renal impairment	56.82	47.96	22	441	88333	63400226

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Taste disorder	43.68	40.97	11	370	7144	34949406

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Taste disorder	91.59	44.08	23	789	15800	79727776
Renal impairment	68.96	44.08	33	779	157750	79585826
Ataxia	63.38	44.08	19	793	25020	79718556
Disease progression	58.34	44.08	31	781	184331	79559245
Blood creatinine increased	54.53	44.08	28	784	155029	79588547

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EX14	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
CHEBI has role	CHEBI:33282	bactericides
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62434	ALK inhibitor
CHEBI has role	CHEBI:68495	Type I cell-death inducers
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Reactive oxygen species 1 positive non-small cell lung cancer	indication	72242500
Solid neoplasm with neurotrophic receptor tyrosine kinase gene fusion	indication	786710002

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.61	acidic
pKa2	12.21	acidic
pKa3	8.43	Basic
pKa4	1.79	Basic
pKa5	1.11	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	8673893	July 8, 2028	TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	8673893	July 8, 2028	TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	9255087	July 8, 2028	TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	9255087	July 8, 2028	TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	9616059	July 8, 2028	TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	9649306	May 22, 2033	TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	9649306	May 22, 2033	TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	10231965	Feb. 17, 2035	TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	10231965	Feb. 17, 2035	TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	10561651	Feb. 19, 2035	TREATMENT OF NEUROBLASTOMAS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2024	NEW CHEMICAL ENTITY
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2026	INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION WITHOUT A KNOWN ACQUIRED RESISTENACE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE EITHER PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
100MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2026	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ROS1-POSITIVE
200MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2024	NEW CHEMICAL ENTITY
200MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2026	INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION WITHOUT A KNOWN ACQUIRED RESISTENACE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE EITHER PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
200MG	ROZLYTREK	GENENTECH INC	N212725	Aug. 15, 2019	RX	CAPSULE	ORAL	Aug. 15, 2026	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ROS1-POSITIVE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN	INHIBITOR	IC50	9	SCIENTIFIC LITERATURE	DRUG LABEL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	IC50	7.92	SCIENTIFIC LITERATURE	DRUG LABEL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN	INHIBITOR	IC50	8.52	SCIENTIFIC LITERATURE	DRUG LABEL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN	INHIBITOR	IC50	8.30	SCIENTIFIC LITERATURE	DRUG LABEL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN	INHIBITOR	IC50	8.15	SCIENTIFIC LITERATURE	DRUG LABEL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		IC50	6.85	CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		IC50	6.95	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		IC50	6.67	CHEMBL
Protein-tyrosine kinase 6	Kinase	Q13882	PTK6_HUMAN		IC50	6.71	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		IC50	6.46	CHEMBL

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External reference:

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ID	Source
YMX	PDB_CHEM_ID
018089	NDDF
10132	INN_ID
2197862	RXNORM
25141092	PUBCHEM_CID
322129	MMSL
37312	MMSL
4038664	VANDF
789356007	SNOMEDCT_US
789364001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-091	CAPSULE	100 mg	ORAL	NDA	30 sections
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-091	CAPSULE	100 mg	ORAL	NDA	30 sections
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-091	CAPSULE	100 mg	ORAL	NDA	30 sections
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-094	CAPSULE	200 mg	ORAL	NDA	30 sections
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-094	CAPSULE	200 mg	ORAL	NDA	30 sections
Rozlytrek	HUMAN PRESCRIPTION DRUG LABEL	1	50242-094	CAPSULE	200 mg	ORAL	NDA	30 sections

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