Inavolisib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

About Inavolisib

Inavolisib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2024. Its mechanism of action is classified as Phosphoinositide 3-Kinase alpha Inhibitors. DrugCentral lists 4 molecular targets, including PIK3CA, PIK3CD and PIK3CG. Recorded indications include Locally advanced or metastatic breast cancer.

Indications & contraindications

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

Indications (1)

• Locally advanced or metastatic breast cancer

Mechanism & targets

• Mechanism of action (MoA): Phosphoinositide 3-Kinase alpha Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (4)

Target	Gene	Action	Activity
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	PIK3CA	inhibitor	IC50 10.42
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	PIK3CD	inhibitor	Ki 7.91
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	PIK3CG	inhibitor	Ki 7.74
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	PIK3CB	inhibitor	Ki 7.00

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2025-07-18	EMA	—	Roche Registration GmbH
2024-10-10	FDA	—	Genentech (Roche)

ATC classification

ATC code	Therapeutic hierarchy
L01EM06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Phosphatidylinositol-3-kinase (Pi3K) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ERBB2, ESR1, ESR2, PIK3CA · Testing Required
• FDA label: ERBB2, ESR1, ESR2, PIK3CA · Testing Required
• HCSC label: ERBB2, ESR1, ESR2, PIK3CA · 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
Hyperglycaemia	392.8
Blood glucose increased	131.7

Chemical structure

• Molecular formula: —
• Molecular weight: —
• CAS number: —
• InChIKey: SGEUNORSOZVTOL-CABZTGNLSA-N
• PubChem CID: 124173720

C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](COC4=O)C(F)F

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