Ripretinib

CHEMBL4216467 Phase 4 Approuvé Small molecule

Half-Life

—

Bioavailability

—

Protein Binding

—

Molecular Weight

510.4 g/mol

LogP

4.1

Phase

4

Ripretinib is a switch-control kinase inhibitor that broadly inhibits KIT and PDGFRA kinase activity regardless of mutation type through a dual mechanism of allosterically locking the activation loop in an inactive conformation and blocking ATP binding, overcoming resistance mutations at multiple sites. It is approved for the treatment of advanced gastrointestinal stromal tumors (GIST) that have progressed on prior treatment including imatinib.

Masse moléculaire

510,4000 g/mol

LogP

4,10

TPSA

86,40 Å²

Règle des 5 de Lipinski

Conforme

Aires thérapeutiques

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Non-Small Cell Lung Cancer Breast Cancer Prostate Cancer Colorectal Cancer

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Structure 2D

SVG PNG

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SMILES

CCn1c(=O)c(-c2cc(NC(=O)Nc3ccccc3)c(F)cc2Br)cc2cnc(NC)cc21

InChI

InChI=1S/C24H21BrFN5O2/c1-3-31-21-12-22(27-2)28-13-14(21)9-17(23(31)32)16-10-20(19(26)11-18(16)25)30-24(33)29-15-7-5-4-6-8-15/h4-13H,3H2,1-2H3,(H,27,28)(H2,29,30,33)

Molecular Formula

C24H21BrFN5O2

HBD / HBA

3 / 5

Liaisons Rotatives

5

Atomes Lourds

33

No targets recorded

Target interaction data is not yet available for this drug.

No interactions recorded

Drug interaction data is not yet available for this compound.

No side effects recorded

Side effect data is not yet available for this drug.

Foire aux questions

Ripretinib is a switch-control kinase inhibitor that broadly inhibits KIT and PDGFRA kinase activity regardless of mutation type through a dual mechanism of allosterically locking the activation loop in an inactive conformation and blocking ATP binding, overcoming resistance mutations at multiple sites. It is approved for the treatment of advanced gastrointestinal stromal tumors (GIST) that have progressed on prior treatment including imatinib.

Yes, Ripretinib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

ChEMBL — European Bioinformatics Institute (EBI). CHEMBL4216467. Open-access bioactivity database.
PubChem — National Center for Biotechnology Information (NCBI). CID 71584930. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

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Structure

Données Clés

Formule: C24H21BrFN5O2
Synonymes: 1

Liens externes

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Avertissement médical

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.