Overview
Inavolisib (GDC-0077) is under investigation in clinical trial NCT03006172 (To Evaluate the Safety, Tolerability, and Pharmacokinetics of GDC-0077 Single Agent in Participants With Solid Tumors and in Combination With Endocrine and Targeted Therapies in Participants With Breast Cancer).
Indication
No indication information available.
Associated Conditions
No associated conditions information available.
Research Report
Inavolisib Report
Name: Inavolisib Name (English): Inavolisib DrugBank ID: DB15275 Type: Small Molecule CAS Number: 2060571-02-8
Mechanism of Action: Inavolisib is a selective inhibitor of the Class I PI3Kα isoform (p110α). It binds to the ATP-binding site of PI3Kα, inhibiting the phosphorylation of phosphatidylinositol-4,5-bisphosphate (PIP2) to phosphatidylinositol-3,4,5-trisphosphate (PIP3). This reduces downstream activation of AKT and ribosomal protein S6, leading to decreased cell proliferation, metabolism, and angiogenesis. Inavolisib also specifically triggers the degradation of the mutant p110α protein.
Indication: Inavolisib is indicated in combination with palbociclib and fulvestrant for the treatment of adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy.
Contraindications: There are no specific contraindications listed beyond potential hypersensitivity to the drug or any of its components. Caution should be exercised in patients with a history of diabetes or kidney disease.
Pharmacokinetics:
- Absorption: The absolute oral bioavailability of inavolisib is 76%. Steady-state is reached by approximately day 5, with a Tmax of 3 hours. Food does not significantly affect pharmacokinetics.
- Distribution: Not specified in detail but it crosses cell membranes.
- Metabolism: Inavolisib appears metabolically stable in hepatocytes.
- Elimination: The total clearance of inavolisib is 8.8 L/h. It is a substrate of P-gp and BCRP/ABCG2 transporters.
Side Effects: Common side effects include:
- Neutropenia
- Thrombocytopenia
- Anemia
- Hyperglycemia
- Stomatitis
- Diarrhea
- Nausea
- Rash
- Decreased appetite
- Fatigue
- Headache
- COVID-19 infection
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/07/08 | Not Applicable | Not yet recruiting | |||
2025/01/24 | Phase 3 | Recruiting | |||
2024/07/11 | Phase 1 | Recruiting | |||
2023/06/08 | Phase 3 | Recruiting | |||
2023/05/17 | Phase 3 | Recruiting | |||
2023/02/01 | Phase 2 | Active, not recruiting | MedSIR | ||
2022/12/12 | Phase 3 | Active, not recruiting | |||
2022/04/18 | Phase 2 | Recruiting | |||
2022/03/31 | Phase 2 | Recruiting | German Breast Group | ||
2021/06/18 | Phase 2 | Active, not recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| ITOVEBI inavolisib 9 mg film-coated tablet blister pack | 446751 | Medicine | A | 3/26/2025 | |
| ITOVEBI inavolisib 3 mg film-coated tablet blister pack | 446750 | Medicine | A | 3/26/2025 |
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