Larotrectinib hydrochloride

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H22F2N6O2.ClH
Molecular Weight	464.896
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of Larotrectinib hydrochloride

Structure Search

SMILES

Cl.O[C@H]1CCN(C1)C(=O)NC2=C3N=C(C=CN3N=C2)N4CCC[C@@H]4C5=CC(F)=CC=C5F

InChI

InChIKey=UIHKJNYGFOAQDS-QLOBERJESA-N

InChI=1S/C21H22F2N6O2.ClH/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27;/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31);1H/t14-,18+;/m0./s1

HIDE SMILES / InChI

Molecular Formula	C21H22F2N6O2
Molecular Weight	428.4352
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT02576431 | https://clinicaltrials.gov/ct2/show/NCT02637687 | https://www.ncbi.nlm.nih.gov/pubmed/26216294

Larotrectinib (previously known as ARRY-470 and LOXO-101) is a potent, oral and selective investigational new drug in clinical development for the treatment of patients with cancers that harbor abnormalities involving the tropomyosin receptor kinases (TRKs). Larotrectinib is in phase II clinical trials for the treatment patients with solid tumors, non-Hodgkin lymphoma and for the pediatric patients with advanced solid or primary CNS tumors.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Nerve growth factor receptor Trk-A 15 Target ID: CHEMBL2815 Sources: https://www.loxooncology.com/docs/presentations/LOXO101_EORTC2014_Poster.pdf	Inhibitor 8504	20.0 nM [IC50]
Neurotrophic tyrosine kinase receptor type 2 14 Target ID: CHEMBL4898 Sources: https://www.loxooncology.com/docs/presentations/LOXO101_EORTC2014_Poster.pdf	Inhibitor 8504	20.0 nM [IC50]
NT-3 growth factor receptor 9 Target ID: CHEMBL5608 Sources: https://www.loxooncology.com/docs/presentations/LOXO101_EORTC2014_Poster.pdf	Inhibitor 8504	20.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Solid tumors 147 Sources: https://clinicaltrials.gov/ct2/show/NCT02576431	Primary	Approved 8583	VITRAKVI Approved Use Vitrakvi is specifically indicated for the treatment of adult and pediatric patients with solid tumors that: • have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, • are metastatic or where surgical resection is likely to result in severe morbidity, and • have no satisfactory alternative treatments or that have progressed following treatment. Launch Date 2018
Central nervous system neoplasms 4 Sources: https://clinicaltrials.gov/ct2/show/NCT02637687	Primary	Phase II 1147	Unknown Approved Use Unknown
Non-Hodgkin's lymphoma 81 Sources: https://clinicaltrials.gov/ct2/show/NCT03213704	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
788 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211710s000lbl.pdf	100 mg 2 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		LAROTRECTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
4351 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211710s000lbl.pdf	100 mg 2 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		LAROTRECTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.9 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211710s000lbl.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		LAROTRECTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
100 mg 2 times / day steady, oral Recommended Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	unhealthy, 28 - 82 years Health Status: unhealthy Age Group: 28 - 82 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	Other AEs: Fatigue, Pyrexia... Other AEs: Fatigue (all grades, 37%) Pyrexia (all grades, 18%) Edema peripheral (all grades, 15%) Nausea (all grades, 29%) Vomiting (all grades, 26%) Constipation (all grades, 23%) Diarrhea (all grades, 22%) Abdominal pain (all grades, 13%) Dizziness (all grades, 28%) Headache (all grades, 14%) Cough (all grades, 26%) Dyspnea (all grades, 18%) Nasal congestion (all grades, 10%) Fatigue (grade 3-4, 3%) Pyrexia (grade 3-4, 1%) Nausea (grade 3-4, 1%) Vomiting (grade 3-4, 1%) Constipation (grade 3-4, 1%) Diarrhea (grade 3-4, 2%) Abdominal pain (grade 3-4, 2%) Dizziness (grade 3-4, 1%) Dyspnea (grade 3-4, 2%) Weight increased (all grades, 15%) Arthralgia (all grades, 14%) Myalgia (all grades, 14%) Muscular weakness (all grades, 13%) Back pain (all grades, 12%) Pain in extremity (all grades, 12%) Decreased appetite (all grades, 13%) Decreased appetite (all grades, 11%) Weight increased (grade 3-4, 4%) Arthralgia (grade 3-4, 1%) Myalgia (grade 3-4, 1%) Back pain (grade 3-4, 1%) Pain in extremity (grade 3-4, 1%) Decreased appetite (grade 3-4, 2%) Decreased appetite (grade 3-4, 2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf
100 mg 2 times / day steady, oral Recommended Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	unhealthy, 28 - 82 years Health Status: unhealthy Age Group: 28 - 82 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	Other AEs: ALT increased, AST increased... Other AEs: ALT increased (all grades, 45%) AST increased (all grades, 45%) Hypoalbuminemia (all grades, 35%) Alkaline phosphatase increased (all grades, 30%) Anemia (all grades, 42%) Neutropenia (all grades, 23%) ALT increased (grade 3-4, 3%) AST increased (grade 3-4, 3%) Hypoalbuminemia (grade 3-4, 2%) Alkaline phosphatase increased (grade 3-4, 3%) Anemia (grade 3-4, 10%) Neutropenia (grade 3-4, 7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf
100 mg 2 times / day steady, oral Recommended Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	unhealthy, 28 - 82 years Health Status: unhealthy Age Group: 28 - 82 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf	Disc. AE: Brain edema, Intestinal perforation... Other AEs: Fatigue, Nausea... AEs leading to discontinuation/dose reduction: Brain edema (1 - 2) Intestinal perforation (1 - 2) Pericardial effusion (1 - 2) Pleural effusion (1 - 2) Small intestinal obstruction (1 - 2) Dehydration (1 - 2) Fatigue (1 - 2) ALT increased (1 - 2) AST increased (1 - 2) Enterocutaneous fistula (1 - 2) Amylase increased (1 - 2) Lipase increased (1 - 2) Muscular weakness (1 - 2) Abdominal pain (1 - 2) Asthenia (1 - 2) Decreased appetite (1 - 2) Dyspnea (1 - 2) Hyponatremia (1 - 2) Jaundice (1 - 2) Syncope (1 - 2) Vomiting (1 - 2) Nausea (1 - 2) Acute myeloid leukemia (1 - 2) Other AEs: Fatigue (>20) Nausea (>20) Dizziness (>20) Vomiting (>20) Anemia (>20) AST increased (>20) Cough (>20) ALT increased (>20) Constipation (>20) Diarrhea (>20) ALT increased (6%) AST increased (6%) Dizziness (3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210861s000lbl.pdf
150 mg 2 times / day steady, oral Higher than recommended Dose: 150 mg, 2 times / day Route: oral Route: steady Dose: 150 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	DLT: Alanine aminotransferase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Alanine aminotransferase increased (1 patient) Aspartate aminotransferase increased (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/
200 mg 2 times / day steady, oral Highest studied dose Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	DLT: Dizziness... Dose limiting toxicities: Dizziness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/
200 mg 2 times / day steady, oral Highest studied dose Dose: 200 mg, 2 times / day Route: oral Route: steady Dose: 200 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf
100 mg 2 times / day steady, oral Recommended Dose: 100 mg, 2 times / day Route: oral Route: steady Dose: 100 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/	DLT: Dizziness... Dose limiting toxicities: Dizziness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/30624546/

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 inhibitor 2252 substrate 1946	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
BCRP 910 BSEP 550 CYP1A2 2153 CYP2B6 926 CYP2C19 2057 CYP2C8 1057 MATE1 415 MATE2 267 OAT1 725 OAT3 747 OATP1B1 1079 OATP1B3 961 OCT1 620 OCT2 779 P-gp 1741	BCRP 697 OAT1 395 OAT3 391 OATP1B1 503 OATP1B3 435 OCT1 393 OCT2 434 P-gp 2052	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf#page=95 Page: 95.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
MATE2 267	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 95.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf#page=95 Page: 95.0	yes
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0	yes	yes (co-administration study) Comment: larotrectinib increased midazolam both AUC and Cmax by 1.7-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 94.0

Drug as victim

Target	Modality	Activity	Clinical evidence
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	no
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94	yes [Km >300 uM]
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94, 106	yes [Km >300 uM]	yes (co-administration study) Comment: rifampin increased larotrectinib AUC by 1.7-fold and Cmax by 1.8-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 93, 94, 106
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf#page=95 Page: 95, 104, 105	yes	yes (co-administration study) Comment: coadministration with midazolam increased midazolam AUC and Cmax by 1.7-fold; itraconazole increased larotrectinib AUC by 4.3-fold and Cmax by 2.8-fold; rifampin decreased larotrectinib AUC by 81% and Cmax by 71% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf#page=95 Page: 95, 104, 105

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210861Orig1s000_211710Orig1s000MultidisciplineR.pdf Page: 44, 51, 182

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00171P	https://www.aablocks.com/goods/Goods/detail?id=AA00171P
Aaron Chemicals	AR0017TH	http://www.aaronchem.com/1223403-58-4
abcr GmbH	AB463081	http://www.abcr.com/shop/en/AB463081
AbMole Bioscience	M6151	http://www.abmole.com/products/loxo-101.html
Acorn PharmaTech	ACN-043424	http://www.acornpharmatech.com/
BioChemPartner	BCP16262	http://www.biochempartner.com/1223403-58-4-BCP16262
Chem Scene	CS-5722	http://www.chemscene.com/1223403-58-4.html
Chemspace	CSSB00025704742	https://chem-space.com/CSSB00025704742
DC Chemicals	DC22338	http://www.dcchemicals.com/product_show-DC22338.html
eNovation Chemicals	D572361	https://www.enovationchem.com/ProductDetails.asp?ProductID=D572361
Excenen	EX-A1981	https://www.excenen.com/searchresultlist.php?id=1223403-58-4
Huateng Pharma	F99712	http://en.huatengsci.com/product/Larotrectinib.html
Lab Network	LN01343982	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343982
MedChem Express	HY-12866	https://www.medchemexpress.com/LOXO-101.html
Selleck Chemicals	S5860	http://www.selleckchem.com/products/larotrectinib.html
Smolecule	S002173	http://www.smolecule.com/products/s002173
Smolecule	S532504	http://www.smolecule.com/products/s532504
THE BioTek	bt-253135	https://www.thebiotek.com/product/inhibitors/bt-253135
THE BioTek	bt-272566	https://www.thebiotek.com/product/inhibitors/bt-272566

PubMed

Title	Date	PubMed
Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer.	2013 Nov	24162815
An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101.	2015 Oct	26216294
Targeting NTRK fusion in non-small cell lung cancer: rationale and clinical evidence.	2017 Jun	28444624
Rapid Response to Larotrectinib (LOXO-101) in an Adult Chemotherapy-Naive Patients With Advanced Triple-Negative Secretory Breast Cancer Expressing ETV6-NTRK3 Fusion.	2018 Jun	29233640

Sample Use Guides

In Vivo Use Guide

Oral capsule of LOXO-101 (ARRY-470 (FREE BASE)) - 100mg BID

Route of Administration: Oral

In Vitro Use Guide

ARRY-470 is a selective kinase inhibitor with nanomolar activity against TRKA/B/C but no other significant kinase inhibition below 1000nM. Treatment of cells expressing MPRIP- or CD74-NTRK1 with ARRY-470, CEP-701 and, to a lesser extent, crizotinib, inhibited autophosphorylation of RIP-TRKA and CD74-TRKA. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 16:29:40 GMT 2025` Edited by `admin` on `Wed Apr 02 16:29:40 GMT 2025`
Record UNII	E4BVS4JUA7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, hydrochloride (1:1), (3S)-

Preferred Name

English

Larotrectinib hydrochloride

Common Name

English

Code System Code Type Description

FDA UNII

E4BVS4JUA7

Created by admin on Wed Apr 02 16:29:40 GMT 2025 , Edited by admin on Wed Apr 02 16:29:40 GMT 2025

PRIMARY

CAS

1919868-83-9

Created by admin on Wed Apr 02 16:29:40 GMT 2025 , Edited by admin on Wed Apr 02 16:29:40 GMT 2025

PRIMARY

PUBCHEM

121333501

Created by admin on Wed Apr 02 16:29:40 GMT 2025 , Edited by admin on Wed Apr 02 16:29:40 GMT 2025

PRIMARY

Related Record Type Details


					PF9462I9HX

LAROTRECTINIB

PARENT -> SALT/SOLVATE

Amount:

Details

SMILES

InChI

DescriptionSources: https://clinicaltrials.gov/ct2/show/NCT02576431 | https://clinicaltrials.gov/ct2/show/NCT02637687 | https://www.ncbi.nlm.nih.gov/pubmed/26216294

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Approved Use

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Sample Use Guides

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT02576431 | https://clinicaltrials.gov/ct2/show/NCT02637687 | https://www.ncbi.nlm.nih.gov/pubmed/26216294

C_max

T_1/2

Drug as perpetrator