Larotrectinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Larotrectinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2018. Its mechanism of action is classified as Tropomyosin Receptor Kinases Inhibitors. DrugCentral lists 5 molecular targets, including NTRK1, NTRK2 and NTRK3. Recorded indications include Malignant Neoplasm and NTRK fusion gene-positive advanced or recurrent solid tumors.

• Approval status: onp (first approved 2018 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Tropomyosin Receptor Kinases Inhibitors.
• Molecular targets: NTRK1, NTRK2, NTRK3 and ROS1 (5 listed in DrugCentral).
• Indications: Malignant Neoplasm and NTRK fusion gene-positive advanced or recurrent solid tumors.
• ATC code: L01EX12 (Other protein kinase inhibitors).
• Molecular formula: C21H22F2N6O2; molecular weight 428.44 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Malignant Neoplasm
• NTRK fusion gene-positive advanced or recurrent solid tumors

Mechanism & targets

• Mechanism of action (MoA): Tropomyosin Receptor Kinases Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (5)

Target	Gene	Action	Activity
High affinity nerve growth factor receptor	NTRK1	inhibitor	IC50 8.19
BDNF/NT-3 growth factors receptor	NTRK2	inhibitor	IC50 8.09
NT-3 growth factor receptor	NTRK3	inhibitor	IC50 7.97
Proto-oncogene tyrosine-protein kinase ROS	ROS1	unknown	IC50 7.63
Activated CDC42 kinase 1	TNK2	unknown	IC50 6.24

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2021-03-23	PMDA	—	Bayer Yakuhin, Ltd.	Yes
2019-09-19	EMA	—	Bayer AG	Yes
2018-11-26	FDA	—	LOXO ONCOLOGY INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX12	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: NTRK1, NTRK2, NTRK3 · Testing Required
• FDA label: NTRK1, NTRK2, NTRK3 · Testing Required
• HCSC label: NTRK1, NTRK2, NTRK3 · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Disease progression	47.3
Neuropathy peripheral	46.8
Drug resistance	38.2
Malignant neoplasm progression	36.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Larotrectinib is on its molecule page.

• Molecular formula: C₂₁H₂₂F₂N₆O₂
• Molecular weight: 428.44 g/mol
• CAS number: 1223403-58-4
• InChIKey: NYNZQNWKBKUAII-KBXCAEBGSA-N
• PubChem CID: 46188928

O[C@H]1CCN(C1)C(=O)NC1=C2N=C(C=CN2N=C1)N1CCC[C@@H]1C1=CC(F)=CC=C1F

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Larotrectinib used for?

DrugCentral lists the following indications for Larotrectinib: Malignant Neoplasm and NTRK fusion gene-positive advanced or recurrent solid tumors.

How does Larotrectinib work?

Larotrectinib is classified as Tropomyosin Receptor Kinases Inhibitors; its molecular targets in DrugCentral include NTRK1 (inhibitor), NTRK2 (inhibitor), NTRK3 (inhibitor) and ROS1.

When was Larotrectinib first approved?

Larotrectinib was first approved by the FDA in 2018.

What drug class does Larotrectinib belong to?

Larotrectinib is in the Kinase Inhibitor class.

What is the chemical formula of Larotrectinib?

Larotrectinib has the molecular formula C21H22F2N6O2 and a molecular weight of 428.44 g/mol.

Sources

• DrugCentral drug card 5305 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3889654 — compound record and bioactivity
• PubChem CID 46188928 — chemical identifiers
• DrugBank DB14723 — drug record
• FDA UNII PF9462I9HX — substance identity
• DailyMed: FDA labels for Larotrectinib — current prescribing information (label search)
• UniProt P04629 (NTRK1) — target protein
• UniProt Q16620 (NTRK2) — target protein
• UniProt Q16288 (NTRK3) — target protein
• UniProt P08922 (ROS1) — target protein
• UniProt Q07912 (TNK2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.