Alpelisib

CHEMBL2396661 Phase 4 Approuvé Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
441.5 g/mol
LogP
3.2
Phase
4

A targeted cancer therapy that blocks PI3K-alpha, a specific enzyme that is often overactive due to PIK3CA gene mutations and drives the growth of certain breast, colorectal, and bladder cancers. By interrupting this signaling pathway, alpelisib can slow tumor growth, particularly in hormone receptor-positive, HER2-negative breast cancer.

Masse moléculaire

441,5000 g/mol

LogP

3,20

TPSA

129,00 Ų

Règle des 5 de Lipinski

Conforme

Aires thérapeutiques

Mécanisme d'action

Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mécanisme

Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

Structure 2D

SVG PNG

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SMILES

Cc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1ccnc(C(C)(C)C(F)(F)F)c1

InChI

InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1

Molecular Formula

C19H22F3N5O2S

HBD / HBA

2 / 8

Liaisons Rotatives

4

Atomes Lourds

30

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

A targeted cancer therapy that blocks PI3K-alpha, a specific enzyme that is often overactive due to PIK3CA gene mutations and drives the growth of certain breast, colorectal, and bladder cancers. By interrupting this signaling pathway, alpelisib can slow tumor growth, particularly in hormone receptor-positive, HER2-negative breast cancer.

Targets the HER2 (ErbB2) receptor tyrosine kinase, blocking HER2-mediated signaling that drives proliferation in HER2-overexpressing cancer cells.

Yes, Alpelisib 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). CHEMBL2396661. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 56649450. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.

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.