marked.bio

PI3Kα inhibitor · small molecule

inavolisib

15 active trials across 8 of our biomarkers, targeting PI3Kα. 2 active approvals for a biomarker on marked.bio.

Also known as GDC-0077, Itovebi.

Counts only trials that select patients by one of the biomarkers on marked.bio, not every trial of this drug.

Approvals and pivotal results

Biomarker-selected approvals in the United States and the European Union, with the pivotal trial's results and side effects where we have them. Results from different trials are not directly comparable.

TherapyBiomarkerTumourUnited StatesEuropean Union
inavolisib with palbociclib + fulvestrant
EU (EMA), 2025
PIK3CA-mutated, locally advanced or metastatic, recurrence on or within 12 months of completing adjuvant endocrine therapy EU marketing authorisation 18/07/2025. Source
Itovebipalbociclib pagefulvestrant page 		PIK3CA activating mutation breast (ER+/HER2-) Not approved Approved 2025

INAVO120 vs placebo + palbociclib + fulvestrant, 325 randomised (1:1)
PFS 15.0 months vs 7.3 months, HR 0.43 (0.32-0.59)Response 58% vs 25%

Trial details and side effects
Patients
PIK3CA-mutated, endocrine-resistant HR+/HER2- breast cancer (NCT04191499)
Most common side effects
low neutrophils, low haemoglobin, high fasting glucose, low platelets, stomatitis, diarrhoea, fatigue, nausea, rash, decreased appetite
Notes
EU figures from the EPAR summary; trial details and side effects from the US approval.
Source
EU summary (EPAR)
inavolisib with palbociclib + fulvestrant
FDA, 2024
endocrine-resistant, PIK3CA-mutated, locally advanced or metastatic, recurrence on or after adjuvant endocrine therapy FDA approval 10/10/2024; companion test FoundationOne Liquid CDx. Source
Itovebipalbociclib pagefulvestrant page 		PIK3CA activating mutation breast (HR+/HER2-) Approved 2024 Not approved

INAVO120 vs placebo + palbociclib + fulvestrant, 325 randomised (1:1)
PFS 15.0 months vs 7.3 months, HR 0.43 (0.32-0.59)Response 58% vs 25%OS HR 0.64 (0.43-0.97), interim

Trial details and side effects
Patients
PIK3CA-mutated, endocrine-resistant HR+/HER2- breast cancer (NCT04191499)
Most common side effects
low neutrophils, low haemoglobin, high fasting glucose, low platelets, stomatitis, diarrhoea, fatigue, nausea, rash, decreased appetite
Notes
FDA approval summary (2024); later OS analysis reported a significant benefit (published 2025, not yet in our data).
Source
FDA approval summary

Biomarkers

BiomarkerActive trialsAll trialsFurthest active phase
PIK3CA activating mutation 13 15 Phase 3
BRCA1/2 mutation 1 1 Phase 2
HER2 (ERBB2) activating mutation 1 1 Phase 2
KRAS G12C 1 1 Phase 1
ALK fusion 0 1 –
BRAF V600E 0 1 –
MSI-H / dMMR 0 1 –
RET fusion or mutation 0 1 –

Sponsors

Industry sponsors leading active biomarker-selected trials of inavolisib.

  1. Roche 9

Trials

15 of 17 trials shown

  1. 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

    Recruiting Phase 3 Roche Started 2025Primary completion 2032-01 NCT06790693

    inavolisib FDA EUCDK4/6iletrozole

    …and Letrozole vs Placebo + CDK4/6i and Letrozole in Participants With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer

    PIK3CA activating mutationBreast Cancer

  2. 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

    Recruiting Phase 3 Roche Started 2023Primary completion 2026-12 NCT05894239

    inavolisib FDA EUPhesgoTaxane-based ChemotherapyOptional Endocrine Therapy of Investigator's Choice

    Confirmation of PIK3CA-mutation biomarker eligibility based on valid results from central testing of tumor tissue documen…

    PIK3CA activating mutationMetastatic Breast Cancer

  3. 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

    Recruiting Phase 3 Roche Started 2023Primary completion 2026-11 NCT05646862

    inavolisib FDA EUfulvestrant FDA EUalpelisib FDA EUBupropionOmeprazolemidazolam

    …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 Ther…

    PIK3CA activating mutationBreast Cancer

  4. 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

    Active, not recruiting Phase 2/3 Roche Started 2020Primary completion 2023-09 NCT04191499

    inavolisib FDA EUpalbociclib FDA EUfulvestrant FDA EU

    …b + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Participants With PIK3CA-Mutant, Hormone Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer

    PIK3CA activating mutationBreast Cancer

  5. Inavolisib for PIK3CA Mutated Advanced Endometrial Cancer: MITO END-4

    Not yet recruiting Phase 2 National Cancer Institute, Naples Started 2026Primary completion 2030-05 NCT07522697

    inavolisib FDA EU

    Biomarker eligibility: valid results from testing of tumor tissue documenting PIK3CA mutations listed below (a-m)

    PIK3CA activating mutationEndometrial Cancer

  6. A Phase ll, Interventional, Single-arm Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib and Fulvestrant in Chinese Patients With PIK3CA-mutant, HR-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer.

    Not yet recruiting Phase 2 Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University Started 2026Primary completion 2028-12 NCT07618390

    inavolisib FDA EUribociclibfulvestrant FDA EU

    …fficacy and Safety of Inavolisib Plus Ribociclib and Fulvestrant in Chinese Patients With PIK3CA-mutant, HR-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer.

    PIK3CA activating mutationBreast Cancer

  7. A Phase II, Single-arm Study to Evaluate the Efficacy and Safety of Inavolisib in Combination With Eribulin in Pretreated Advanced Triple-negative Breast Cancer Harboring a PIK3CA Mutation

    Not yet recruiting Phase 2 Hu Hai Started 2026Primary completion 2028-03 NCT07441512

    inavolisib FDA EUeribulin

    …results from central testing of tumor tissue documenting the presence of a study-eligible PIK3CA mutation.

    PIK3CA activating mutationTNBC - Triple-Negative Breast Cancer, TNBC

  8. To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer

    Recruiting Phase 2 Roche Started 2026Primary completion 2028-10 NCT07368998

    inavolisib FDA EUfulvestrant FDA EU

    Confirmation of biomarker eligibility: presence of \>= 1 study-eligible PIK3CA mutation

    PIK3CA activating mutationBreast Cancer

  9. A Study to Test Inavolisib Treatments in Participants With Early-Stage, PIK3CA-Mutated Breast Cancer

    Recruiting Phase 2 Roche Started 2025Primary completion 2027-07 NCT07054190

    inavolisib FDA EUribociclibletrozolegiredestrant

    Confirmed PIK3CA mutation

    PIK3CA activating mutationBreast Cancer

  10. A Phase II, Multicenter, Open-label Study to Evaluate the Efficacy and Safety of Neoadjuvant Therapy With Inavolisib Plus Pertuzumab and Trastuzumab as Subcutaneous (PH-FDC SC) and 3-week Cycle Nab-paclitaxel for PIK3CA-mutated, HER2+, eBC

    Not yet recruiting Phase 2 Zhimin Shao Started 2025Primary completion 2026-12 NCT07245797

    pertuzumabtrastuzumabnab-paclitaxelinavolisib FDA EU

    HER2+ disease with confirmed ER-status, PR-status, HER2-status, PIK3CA mutation (tumor), Ki-67 value on core biopsy (target lesion).

    PIK3CA activating mutationBreast Cancer

  11. Neoadjuvant Endocrine Therapy +/- the PI3K Inhibitor Inavolisib in HER2+, HR+, PIK3CA Mutant Early Breast Cancer

    Recruiting Phase 2 GBG Forschungs Started 2023Primary completion 2027-01 NCT05306041

    inavolisib FDA EUPHESGOEndocrine therapy

    HR+/HER2+ disease with centrally confirmed ER-status, PR-status, HER2-status, PIK3CA mutation (tumor), Ki-67 value and TILs on core biopsy (target lesion).

    PIK3CA activating mutationHER2-positive Breast Cancer

  12. Genomics Guided Targeted Post-neoadjuvant Therapy in Patients With Early Breast Cancer (COGNITION-GUIDE)

    Recruiting Phase 2 German Cancer Research Center Started 2023Primary completion 2030-03 NCT05332561

    atezolizumabinavolisibipatasertibolaparibsacituzumab govitecantrastuzumabpertuzumab

    Arm 6 (Trastuzumab / Pertuzumab, ERBBB): HER2 exon-20 insertion, Activating HER2-mutation

    HER2 (ERBB2) activating mutationBRCA1/2 mutationEarly-stage Breast Cancer

  13. A Study Evaluating Single-agent Inavolisib, Inavolisib Plus Atezolizumab in PIK3CA-Mutated Cancers

    Active, not recruiting Phase 1 Roche Started 2023Primary completion 2027-07 NCT06496568

    inavolisib FDA EUatezolizumab

    A Study Evaluating Single-agent Inavolisib, Inavolisib Plus Atezolizumab in PIK3CA-Mutated Cancers

    PIK3CA activating mutationPIK3CA-Mutated Cancers

  14. A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-6036 Alone or in Combination in Participants With Advanced or Metastatic Solid Tumors With a KRAS G12C Mutation

    Active, not recruiting Phase 1 Roche Started 2020Primary completion 2027-12 NCT04449874

    divarasibatezolizumabcetuximabbevacizumaberlotinibGDC-1971inavolisib

    Histologically documented advanced or metastatic solid tumor with KRAS G12C mutation.

    KRAS G12CNon-Small Cell Lung Cancer, Colorectal Cancer, Advanced Solid Tumors

  15. 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

    Active, not recruiting Phase 1 Roche Started 2016Primary completion 2026-12 NCT03006172

    inavolisib FDA EUfulvestrant FDA EUletrozolepalbociclib FDA EUmetformintrastuzumabpertuzumab

    Locally advanced, recurrent, or metastatic, PIK3CA mutant, incurable solid tumor malignancy, including breast cancer

    PIK3CA activating mutationBreast Cancer, Solid Tumor