Repotrectinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

About Repotrectinib

Repotrectinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2023. Its mechanism of action is classified as Cytochrome P450 3A4 Inducers, Proto-Oncogene Tyrosine-Protein Kinase ROS1 Inhibitors and Tropomyosin Receptor Tyrosine Kinase A Inhibitors. DrugCentral lists 27 molecular targets, including ROS1, NTRK3 and NTRK2. Recorded indications include Reactive oxygen species 1 positive non-small cell lung cancer.

Indications & contraindications

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

Indications (1)

• Reactive oxygen species 1 positive non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A4 Inducers; Proto-Oncogene Tyrosine-Protein Kinase ROS1 Inhibitors; Tropomyosin Receptor Tyrosine Kinase A Inhibitors; Tropomyosin Receptor Tyrosine Kinase B Inhibitors; Tropomyosin Receptor Tyrosine Kinase C Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (27)

Target	Gene	Action	Activity
Proto-oncogene tyrosine-protein kinase ROS	ROS1	inhibitor	IC50 10.15
NT-3 growth factor receptor	NTRK3	inhibitor	IC50 9.68
BDNF/NT-3 growth factors receptor	NTRK2	inhibitor	IC50 9.53
High affinity nerve growth factor receptor	NTRK1	inhibitor	IC50 9.27
Tyrosine-protein kinase Fyn	FYN	inhibitor	IC50 8.98
Tyrosine-protein kinase JAK2	JAK2	inhibitor	IC50 8.98
ALK tyrosine kinase receptor	ALK	inhibitor	IC50 8.98
Tyrosine-protein kinase Lyn	LYN	inhibitor	IC50 8.78
Tyrosine-protein kinase Yes	YES1	inhibitor	IC50 8.67
Tyrosine-protein kinase Fgr	FGR	inhibitor	IC50 8.52
Tyrosine-protein kinase TXK	TXK	inhibitor	IC50 8.50
NUAK family SNF1-like kinase 1	NUAK1	inhibitor	IC50 8.35
Proto-oncogene tyrosine-protein kinase Src	SRC	inhibitor	IC50 8.28
Epithelial discoidin domain-containing receptor 1	DDR1	inhibitor	IC50 8.24
Focal adhesion kinase 1	PTK2	inhibitor	IC50 8.16
Tyrosine-protein kinase Lck	LCK	inhibitor	IC50 7.73
Tyrosine-protein kinase JAK1	JAK1	inhibitor	IC50 7.72
Non-receptor tyrosine-protein kinase TYK2	TYK2	inhibitor	IC50 7.67
Leukocyte tyrosine kinase receptor	LTK	inhibitor	IC50 7.66
Discoidin domain-containing receptor 2	DDR2	inhibitor	IC50 7.64

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2023-11-15	FDA	—	BRISTOL	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX28	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, ROS1 · Testing Required
• FDA label: NTRK1, NTRK2, NTRK3, ROS1 · Testing Required
• HCSC label

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
Dizziness	50.8

Chemical structure

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

• Molecular formula: —
• Molecular weight: —
• CAS number: —
• InChIKey: FIKPXCOQUIZNHB-WDEREUQCSA-N
• PubChem CID: 135565923

C[C@H]1CNC(=O)C2=C3N=C(N[C@H](C)C4=CC(F)=CC=C4O1)C=CN3N=C2

Sources & how this page is made

This page is compiled automatically from public scientific databases and is refreshed when those sources are re-ingested. It is not written or reviewed by a clinician.

• DrugCentral — structures, indications, targets, approvals (CC BY-SA 4.0)
• FDA Orange Book — patents and exclusivity
• FDA Adverse Event Reporting System (FAERS) — adverse-event signals
• PharmGKB / CPIC — pharmacogenomics
• PubChem — chemical identifiers