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Other names: RG6114; RO7113129
Modality: Phosphoinositide 3-kinase (PI3K) inhibitor
Disease State: PI3K3CA-mutated HR+/HER2- Breast Cancer
Summary
Inavolisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K) with inhibitory activity predominantly against the catalytic alpha subunit p110α (encoded by the phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha [PIK3CA] gene).1
Clinical Trials
Inavolisib
| NCT ID | Study Phase | Enrollment Status | Study Title | |
|---|---|---|---|---|
| NCT07144111 | Phase I | Recruiting | A Study to Evaluate the Effect of Moderate or Severe Hepatic Impairment on the Pharmacokinetics (PK) of Inavolisib | View details |
| NCT04929223 | Phase I | Recruiting | A Study Evaluating the Safety and Efficacy of Targeted Therapies in Subpopulations of Patients With Metastatic Colorectal Cancer (INTRINSIC) | View details |
| NCT07054190 | Phase II | Recruiting | A Study to Test Inavolisib Treatments in Participants With Early-Stage, PIK3CA-Mutated Breast Cancer | View details |
| NCT07368998 | Phase II | Recruiting | To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer | View details |
| NCT07287150 | Phase II | Recruiting | A Study to Test Inavolisib Treatment in Participants With Metastatic Castration-Resistant Prostate Cancer | View details |
| NCT07405801 | Phase II | Recruiting | A Phase II Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib Plus Fulvestrant Versus Placebo Plus Ribociclib Plus Fulvestrant in Participants With Advanced Breast Cancer | View details |
| NCT05894239 | Phase III | Recruiting | A Study to Evaluate the Efficacy and Safety of Inavolisib in Combination With Phesgo Versus Placebo in Combination With Phesgo in Participants With PIK3CA-Mutated HER2-Positive Locally Advanced or Metastatic Breast Cancer | View details |
| NCT06790693 | Phase III | Recruiting | A Study Evaluating the Efficacy and Safety of Inavolisib Plus CDK4/6 Inhibitor and Letrozole vs Placebo + CDK4/6i and Letrozole in Participants With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer | View details |
| NCT06496568 | Phase I | Active, not recruiting | A Study Evaluating Single-agent Inavolisib, Inavolisib Plus Atezolizumab in PIK3CA-Mutated Cancers | View details |
| NCT04191499 | Phase II / Phase III | Active, not recruiting | A Study Evaluating the Efficacy and Safety of Inavolisib + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Participants With PIK3CA-Mutant, Hormone Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer | View details |
| NCT05646862 | Phase III | Active, not recruiting | A Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy | View details |
| NCT03006172 | Phase I | Active, not recruiting | To Evaluate the Safety, Tolerability, and Pharmacokinetics of Inavolisib Single Agent in Participants With Solid Tumors and in Combination With Endocrine and Targeted Therapies in Participants With Breast Cancer | View details |
| NCT03424005 | Phase I / Phase II | Recruiting | A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer | View details |
| NCT04802759 | Phase I / Phase II | Recruiting | A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer | View details |
Proposed Mechanism of Action
Inavolisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα.1
In vitro, inavolisib induced the degradation of mutated PI3K catalytic alpha subunit p110α (encoded by the PIK3CA gene), inhibited phosphorylation of the downstream target protein kinase B (AKT), reduced cellular proliferation, and induced apoptosis in PIK3CA-mutated breast cancer cell lines.1
In vivo, inavolisib reduced tumor growth in PIK3CA-mutated, estrogen receptor (ER)-positive, breast cancer xenograft models.
AKT=Protein kinase B; CDK=Cyclin-dependent kinase; DNA=Deoxyribonucleic acid; E2F=Early 2 factor; FOXO=Forkhead box O; GSK3=Glycogen synthase kinase-3; mTOR1/2=Mechanistic/mammalian target of rapamycin complex 1 and 2; PI3K=Phosphatidylinositol 3-kinase; PDK=Pyruvate dehydrogenase kinase; PIP2=Phosphatidylinositol (4,5)-bisphosphate; PIP3=Phosphatidylinositol (3,4,5)-trisphosphate; PTEN=Phosphatase and tensin homolog; Rb=Retinoblastoma protein; RTK=Receptor tyrosine kinase
1. Vasan N, et al. Ann Oncol. 2019;30(Suppl 10):x3-x11. 2. Mosele F, et al. Ann Oncol. 2020;31(3):377-386. 3. Miller TW, et al. Breast Cancer Res. 2011;13(6):224. 4. Hong R, et al. Cancer Res. 2018;78(4 Suppl):Abstract nr PD4-14. 5. Edgar K, et al. Cancer Res. 2020;80(4 Suppl):Abstract nr P3-11-23.
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mBC
metastatic breast cancer -
PI3K
phosphatidylinositol 3-kinase