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Inavolisib

Phase 3

Breast Cancer | Small molecule | Oncology |Roche Holding AG|Last Updated: Sep 3, 2026

Target and mechanism

Molecular targetPIK3CA
Target classInhibitor
ModalitySmall molecule
ChEMBLCHEMBL4650215

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindCONTROLLEDDMC
Total Trials8
Total Enrollment1,655

FDA Designations

No designations recorded

Clinical trial landscape

Inavolisib · 14 trials · 9 indications

Phase 3 3Phase 2 7Phase 1 4
NCT06790693A 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 CancerBreast Cancer
RECRUITING450 Analytics
NCT05894239A 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 CancerMetastatic Breast Cancer
RECRUITING230 Analytics
NCT05646862A 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 TherapyBreast Cancer
RECRUITING420 Analytics
PHASE3RECRUITING
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
Breast Cancer
NCT06790693450
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PHASE3RECRUITING
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
Metastatic Breast Cancer
NCT05894239230
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PHASE3RECRUITING
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
Breast Cancer
NCT05646862420
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Study Endpoints

Primary Endpoints

Progression-Free Survival (PFS)
From randomization to the first occurrence of disease progression or death from any cause, whichever occurs first (up to 7 years)
Investigator-Assessed Progression-Free Survival (PFS)
Up to approximately 40 months
Blinded Independent Central Review (BICR)-Assessed Progression Free Survival (PFS)
From randomization until disease progression or death due to any cause (up to approximately 64 months)
Sub-study: Maximum observed Drug Concentration (Cmax) for Midazolam
Day -4 and -3 of Cycle (C) 1, Day (D) 11 and C1D12. A cycle is 28 days.
Sub-study: Cmax for Bupropion
Day -3, -2, -1 of C1D1, C1D12, C1D13, C1D14 and C1D15. A cycle is 28 days.
Sub-study: Cmax for Omeprazole
Day -4 and -3 of C1D11 and C1D12. A cycle is 28 days.
Sub-study: Area Under the Concentration-Time Curve From Time 0 to Last Measurable Concentration (AUC [0-last]) for Midazolam
Day -4 and -3 of C1D11 and C1D12. A cycle is 28 days.
Sub-study: AUC (0-last) for Bupropion
Day -3, -2, -1 of C1D1, C1D12, C1D13, C1D14 and C1D15. A cycle is 28 days.
Sub-study: AUC (0-last) for Omeprazole
Day -4 and -3 of C1D11 and C1D12. A cycle is 28 days.
Sub-study: Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC [0-infinity]) for Midazolam
Day -4 and -3 of C1D11 and C1D12. A cycle is 28 days.
Sub-study: AUC (0-infinity) for Bupropion
Day -3, -2, -1 of C1D1, C1D12, C1D13, C1D14 and C1D15. A cycle is 28 days.
Sub-study: AUC (0-infinity) for Omeprazole
Day -4 and -3 of C1D11 and C1D12. A cycle is 28 days.
Percentage of Participants With Grade 4 Hyperglycemia Adverse Events (AEs) After Cycle 1
Up to approximately 21 months
Percentage of Participants Hospitalized for Hyperglycemia or its Complications After Cycle 1
Up to approximately 21 months
Percentage of Participants with AEs After Cycle 1
Up to approximately 21 months
Percentage of Participants With Confirmed Objective Response (cORR)
Up to approximately 2 years
Radiographic Progression-free Survival (rPFS)
Up to approximately 5 years
Percentage of Participants With Objective Response Rate (ORR)
Up to approximately 2 years
Percentage of Participants With Treatment Emergent Adverse Events (TEAEs)
Up to approximately 2 years
Percentage of Participants with Adverse Events (AEs)
From first dose up to 30 days after last dose (approximately 8 months)
Pathologic complete response in the breast and axillary lymph nodes (ypT0/is ypN0)
21 weeks (time window + 3 weeks)

Pathological complete response (ypT0/is ypN0) is defined as no microscopic evidence of residual invasive tumor cells in all resected specimens of the breast and axilla.

Maximum Observed Concentration (Cmax) of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
Area Under Curve (AUC) from Hour 0 to the Last Measurable Concentration (AUC [0-t]) of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
AUC from Zero to Infinity (AUC [0-inf]) Extrapolated of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
Geometric Mean Ratio of Cmax of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
Geometric Mean Ratio of AUC (0-t) of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
Geometric Mean Ratio of AUC (0-inf) of Inavolisib
Pre-dose (0 hour), 30 minutes (min), 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, and 96 hours postdose
Percentage of Participants with Select Treatment-related Toxicities (TRT) in Arm B
Day 1 of Cycle 1 to Day 3 of Cycle 2 (each cycle = 21 days)
Percentage of Participants with Adverse Events (AEs) and serious adverse events (SAEs)
From baseline up to approximately 3 years
Objective Response Rate
Approximately 84 months

Defined as the proportion of participants with a complete response or partial response, as determined by the investigator according to RECIST v1.1

Stage 1: Percentage of Participants With Dose Limiting Toxicities
Day 1 up to Day 28 (for Stage 1 Arm A: Day 1 up to Day 35)
Recommended Phase II Dose of Inavolisib
Day 1 up to Day 28 (for Stage 1 Arm A: Day 1 up to Day 35)
Percentage of Participants With Adverse Events and Serious Adverse Events
Day 1 up to 6 years

Secondary Endpoints

Overall Survival (OS)
From randomization to death from any cause (up to 7 years)
Investigator-assessed Objective Response Rate (ORR)
Up to 7 years
Investigator-assessed Duration of Response (DOR)
From the first occurrence of a confirmed objective response to the first occurrence of disease progression or death from any cause, whichever occurs first (up to 7 years)
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Inavolisib + Letrozole + CDK4/6iEXPERIMENTALParticipants will receive inavolisib, letrozole and CDK4/6i.
Placebo + Letrozole + CDK4/6iPLACEBO_COMPARATORParticipants will receive placebo, letrozole and CDK4/6i.
Induction Therapy: Phesgo plus Taxane-Based ChemotherapyOTHERParticipants will be administered the treatments as outlined in the interventions section.
Maintenance Therapy: Inavolisib plus PhesgoEXPERIMENTALParticipants will be administered the treatments as outlined in the interventions section.
Maintenance Therapy: Placebo plus PhesgoACTIVE_COMPARATORParticipants will be administered the treatments as outlined in the interventions section.
Inavolisib + FulvestrantEXPERIMENTALParticipants will be administered the treatments as outlined in the interventions section.
Alpelisib + FulvestrantACTIVE_COMPARATORParticipants will be administered the treatments as outlined in the interventions section.
Sub-study: Inavolisib + Fulvestrant + CYP substratesEXPERIMENTALParticipants will be administered the treatments as outlined in the interventions section.
Inavolisib + Fulvestrant + PalbociclibEXPERIMENTALParticipants will receive inavolisib and fulvestrant (and some participants palbociclib) as outlined in the intervention section.
Inavolisib + Ribociclib + FulvestrantEXPERIMENTALParticipants will receive inavolisib, ribociclib and fulvestrant.
Placebo + Ribociclib + FulvestrantPLACEBO_COMPARATORParticipants will receive placebo, ribociclib and fulvestrant.
Arm 1EXPERIMENTALParticipants will receive Inavolisib plus enzalutamide
Arm 2ACTIVE_COMPARATORParticipants will receive either ARPi switch (enzalutamide or abiraterone) or docetaxel
Inavolisib Dose A plus FulvestrantEXPERIMENTALParticipants will recieve an inavolisib tablet orally (PO) along with fulvestrant as an intramuscular (IM) injection.
Inavolisib Dose B plus FulvestrantEXPERIMENTALParticipants will recieve an inavolisib tablet PO along with fulvestrant as an IM injection.
Arm AEXPERIMENTALParticipants will receive inavolisib and letrozole orally (PO) once a day (QD) from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 1-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and letrozole will be administered PO QD on days 1-21 (each cycle=21 days).
Arm BEXPERIMENTALParticipants will receive a starting regimen of inavolisib and letrozole PO QD from Day 1 to 28 in cycle 1 (each cycle=28 days). Starting on Day 1 of Cycle 2, all participants will receive the triplet regimen inavolisib + ribociclib + letrozole as follows: inavolisib and letrozole PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 2-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and letrozole will be administered PO QD on days 1-21 (each cycle=21 days).
Arm CEXPERIMENTALParticipants will receive a starting regimen of ribociclib PO QD from Day 1 to 21 and letrozole PO QD from Day 1 to 28 in cycle 1 (each cycle=28 days). Starting on Day 1 of Cycle 2, all participants will receive the triplet regimen inavolisib + ribociclib + letrozole as follows: inavolisib and letrozole PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 2-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and letrozole will be administered PO QD on days 1-21 (each cycle=21 days).
Arm D (non-randomized)EXPERIMENTALParticipants will receive inavolisib and letrozole PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 1-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and letrozole will be administered PO QD on days 1-21 (each cycle=21 days).
Arm EEXPERIMENTALParticipants will receive inavolisib and giredestrant PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 1-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and giredestrant will be administered PO QD on days 1-21 (each cycle=21 days).
Arm FEXPERIMENTALParticipants will receive a starting regimen of inavolisib and giredestrant PO QD from Day 1 to 28 in cycle 1 (each cycle=28 days). Starting on Day 1 of Cycle 2, all participants will receive the triplet regimen inavolisib + ribociclib + giredestrant as follows: inavolisib and giredestrant PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 2-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and giredestrant will be administered PO QD on days 1-21 (each cycle=21 days).
Arm GEXPERIMENTALParticipants will receive a starting regimen of ribociclib PO QD from Day 1 to 21 and giredestrant PO QD from Day 1 to 28 in cycle 1 (each cycle=28 days). Starting on Day 1 of Cycle 2, all participants will receive the triplet regimen inavolisib + ribociclib + giredestrant as follows: inavolisib and giredestrant PO QD from Day 1 to 28 and ribociclib PO QD from Day 1 to 21 in cycles 2-5 (each cycle=28 days). In cycle 6, inavolisib, ribociclib and giredestrant will be administered PO QD on days 1-21 (each cycle=21 days).
InavolisibEXPERIMENTALInavolisib for 6 cycles (18 weeks) Neoadjuvant endocrine therapy in combination with dual anti-HER2 blockade consisting of ready-to-use fixed-dose combination of pertuzumab and trastuzumab as subcutaneous (PH-FDC SC) formulation q3w for 6 cycles (18 weeks)
without InavolisibOTHERNeoadjuvant endocrine therapy in combination with dual anti-HER2 blockade consisting of ready-to-use fixed-dose combination of pertuzumab and trastuzumab as subcutaneous (PH-FDC SC) formulation q3w for 6 cycles (18 weeks)
Inavolisib + Palbociclib + FulvestrantEXPERIMENTALParticipants will receive inavolisib, palbociclib, and fulvestrant.
Placebo + Palbociclib + FulvestrantPLACEBO_COMPARATORParticipants will receive placebo, palbociclib, and fulvestrant. Participants randomized to the placebo arm who are still deriving benefit from the study treatment will be given an optional opportunity to crossover to the inavolisib arm.
Cohort 1EXPERIMENTALParticipants with normal hepatic function will receive a single oral dose of inavolisib on Day 1
Cohort 2EXPERIMENTALParticipants with moderate hepatic function will receive a single oral dose of inavolisib on Day 1
Cohort 3EXPERIMENTALParticipants with severe hepatic function will receive a single oral dose of inavolisib on Day 1
Inavolisib + CetuximabEXPERIMENTALParticipants will receive 9 milligrams (mg) of inavolisib by mouth once daily (QD) on Days 8-28 of Cycle 1, then QD on Days 1-28 from Cycle 2 onwards (1 cycle=28 days). Participants will also receive cetuximab intravenous (IV) infusion 400 mg/m2 body surface area on Day 1 of Cycle 1. All subsequent weekly (QW) doses will be 250 mg/m2 each. This arm is closed.
Inavolisib + BevacizumabEXPERIMENTALParticipants will receive 9 mg of inavolisib by mouth QD combined with bevacizumab 15 milligram/kilogram (mg/kg) IV once every three weeks (Q3W) on Day 1 of each cycle (1 cycle=21 days). This arm is closed.
Atezolizumab + Tiragolumab + BevacizumabEXPERIMENTALParticipants in this randomized cohort will receive 1200 mg of atezolizumab by IV infusion on Day 1 of each cycle, combined with tiragolumab at a dose of 600 mg IV infusion on Day 1 of each cycle and bevacizumab IV infusion at a dose of 15 mg/kg on Day 1 of each cycle. (Cycle length=21 days) This arm is active, and not recruiting participants.
Atezolizumab + TiragolumabEXPERIMENTALParticipants in this randomized cohort will receive 1200 mg of atezolizumab by IV infusion on Day 1 of each cycle combined with tiragolumab 600 mg IV infusion on Day 1 of each cycle. (Cycle length=21 days) This arm is active, and not recruiting participants.
Atezolizumab + SY-5609EXPERIMENTALParticipants will receive 1680 mg of atezolizumab by IV infusion on Day 1 of each cycle Q4W in repeated 28-day cycles combined with SY-5609 at a dose of 3, 4, 5, 6, 7 or 10 mg by mouth for 7 days, followed by 7 days off. (Cycle length=28 days) This arm is closed.
Divarasib + Cetuximab + FOLFOXEXPERIMENTALParticipants will receive cetuximab IV 500 mg/m2 body surface area on Days 1 and 15 and FOLFOX on Days 1 and 15 with divarasib PO QD on Days 1-28. (Cycle length=28 days) This arm is recruiting participants.
Divarasib + CetuximabEXPERIMENTALParticipants will receive cetuximab IV 500 mg/m2 body surface area on Days 1 and 15 with divarasib PO QD on Days 1-28. (Cycle length=28 days) This arm is active, and not recruiting participants.
Divarasib + Cetuximab + FOLFIRIEXPERIMENTALParticipants will receive cetuximab IV 500 mg/m2 body surface area on Days 1 and 15 and FOLFIRI on Days 1 and 15 with divarasib PO QD on Days 1-28. (Cycle length=28 days) This arm is active, and not recruiting participants.
Divarasib + Bevacizumab + FOLFOXEXPERIMENTALParticipants will receive Bevacizumab 5 mg/kg by IV infusion on Days 1 and 15 and FOLFOX on Days 1 and 15 with Divarasib PO QD on Days 1-28. (Cycle length=28 days) This arm is recruiting participants.
Divarasib + Bevacizumab + FOLFIRIEXPERIMENTALParticipants will receive Bevacizumab 5 mg/kg by IV infusion on Days 1 and 15 and FOLFIRI on Days 1 and 15 with Divarasib PO QD on Days 1-28. (Cycle length=28 days) This arm is recruiting participants.
Stage I Arm A: Inavolisib Single AgentEXPERIMENTALParticipants will receive inavolisib in escalating dose levels with starting dose of 6 milligrams (mg). Participants will receive single dose of inavolisib on Day 1 of Cycle 1 followed by once daily from Day 8 of Cycle 1. (Cycle length: 35 days for Cycle 1 and 28 days for all other cycles). Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage I Arm B: Inavolisib + Palbociclib + LetrozoleEXPERIMENTALParticipants will receive inavolisib in escalating dose levels (starting dose 3 mg) on Days 1-28, palbociclib on Days 1-21, and letrozole on Days 1-28 of each 28-day cycle. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage I Arm C: Inavolisib + LetrozoleEXPERIMENTALParticipants will receive inavolisib in escalating dose levels along with letrozole on Days 1-28 of each 28-day cycle. The starting dose of inavolisib will not exceed the starting dose in Stage I Arm A. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm B: Inavolisib + Palbociclib + LetrozoleEXPERIMENTALParticipants will receive inavolisib on Days 1-28 in combination with palbociclib on Days 1-21 and letrozole on Days 1-28 of each 28-day cycle. Dose of inavolisib will be decided based on the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm C: Inavolisib + LetrozoleEXPERIMENTALParticipants will receive inavolisib in combination with letrozole on Days 1-28 of each 28-day cycle. Dose of inavolisib will be decided based on the results of Stage I Arm C. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm D: Inavolisib + FulvestrantEXPERIMENTALParticipants will receive inavolisib on Days 1-28 in combination with fulvestrant on Day 1 and 15 of Cycle 1 and then on Day 1 from Cycle 2 (cycle length: 28 days). Dose of inavolisib will be decided based on the results of Stage I Arm C. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm E: Inavolisib + Palbociclib + FulvestrantEXPERIMENTALParticipants will receive inavolisib (Days 1-28) in combination with palbociclib (Days 1-21) and fulvestrant (Days 1 and 15 of Cycle 1; Day 1 for subsequent cycles)(Cycle = 28 days). Dose of inavolisib will be determined from the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm F: Inavolisib + Palbociclib + Fulvestrant + MetforminEXPERIMENTALParticipants will receive inavolisib (Days 1-28) in combination with palbociclib (Days 1-21), fulvestrant (Days 1 and 15 of Cycle 1; Day 1 for subsequent cycles) and metformin (Days 1-28)(Cycle = 28 days). Dose of inavolisib will be determined from the results of Stage I Arm B. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.
Stage II Arm G: Inavolisib + Trastuzumab + PertuzumabEXPERIMENTALParticipants will receive inavolisib in combination with trastuzumab and pertuzumab (Days 1-21). Dose of inavolisib will be determined from the results of Stage I Arm A. Participants will continue treatment until the end of the study in the absence of unacceptable toxicities and unequivocal disease progression.

Interventions

NameTypeDescription
InavolisibDRUGParticipants will receive oral inavolisib once daily (QD).
PlaceboDRUGParticipants will receive oral placebo QD.
CDK4/6iDRUGParticipants will receive CDK4/6i on either Days 1-21 or Days 1-28 of each 28-day cycle.
LetrozoleDRUGParticipants will receive oral letrozole QD.
PhesgoDRUGPhesgo will be administered to participants subcutaneously every 3 weeks (Q3W) on D1 of each 21-day cycle.
Taxane-based ChemotherapyDRUGDuring the induction therapy phase, the investigator's choice of taxane-based chemotherapy will be administered after Phesgo.
Optional Endocrine Therapy of Investigator's ChoiceDRUGOptional endocrine therapy (ET) is allowed at the discretion of the investigator, based on the standard of care. Allowed ETs are tamoxifen, or one of the specified third-generation aromatase inhibitor (AI \[anastrozole, letrozole, or exemestane\]), or fulvestrant. The investigator will determine and supply the appropriate luteinizing hormone-releasing hormone (LHRH) agonist locally approved for use in breast cancer. The LHRH agonist will be administered according to local prescribing information.
FulvestrantDRUGParticipants will be administered 500 mg of fulvestrant on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle of main study and sub-study.
AlpelisibDRUGAlpelisib will be administered to participants at the approved dose in combination with fulvestrant: 300 mg taken PO QD and on days 1-28 of each 28-day cycle.
BupropionDRUGParticipants will be administered bupropion PO on Day -3 and Day 12 of Cycle 1 of the sub-study.
OmeprazoleDRUGParticipants will be administered omerprazole PO on Day -4 and Day 11 of Cycle 1 of sub-study.
MidazolamDRUGParticipants will be administered midazolam PO on Day -4 and Day 11 of Cycle 1 of sub-study.
PalbociclibDRUGSome participants will receive oral palbociclib on Days 1-21 of each 28-day cycle.
RibociclibDRUGRibociclib will be administered as per the schedule mentioned in the protocol.
EnzalutamideDRUGEnzalutamide will be administered orally as per the schedule specified in the protocol.
AbirateroneDRUGAbiraterone will be administered orally as per the schedule specified in the protocol.
DocetaxelDRUGDocetaxel will be administered intravenously as per the schedule specified in the protocol.
GiredestrantDRUGGiredestrant will be administered as per the schedule specified in the arms
Endocrine therapyDRUGEndocrine therapy per physician´s choice with either tamoxifen 20mg or an aromatase inhibitor +/- GnRH analogue for premenopausal women and men
AtezolizumabDRUGParticipants will receive atezolizumab, 1200 mg, as IV infusion Q3W on Day 1 of each 21-day cycle.
BevacizumabDRUGBevacizumab IV will be administered as per schedule specified in the respective arm.
CetuximabDRUGCetuximab IV will be administered as per schedule specified in the respective arm.
TiragolumabDRUGTiragolumab IV infusion will be administered as per schedule specified in the respective arm.
SY-5609DRUGSY-5609 will be administered by mouth as per schedule specified in the respective arm.
DivarasibDRUGDivarasib will be administered orally as per schedule specified in the respective arms.
FOLFOXDRUGFOLFOX (5-fluorouracil, leucovorin, oxaliplatin) IV will be administered as per schedule specified in the respective arm.
FOLFIRIDRUGFOLFIRI (leucovorin, 5-fluorouracil, irinotecan) IV will be administered as per schedule specified in the respective arm.
FoundationOne®Liquid CDxDIAGNOSTIC_TESTFoundationOne®Liquid CDx is used to identify presence of genomic alterations for participant cohort assignment.
MetforminDRUGParticipants will receive oral metformin once daily, starting on Cycle 1, Day 1, as tolerated.
TrastuzumabDRUGParticipants will receive trastuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 8 mg/kg for Cycle 1 and a dose of 6 mg/kg for subsequent cycles, until disease progression or unacceptable toxicity.
PertuzumabDRUGParticipants will receive pertuzumab, administered by IV infusion on Day 1 of each 21-day cycle, at a loading dose of 840 mg for Cycle 1 and a dose of 420 mg for subsequent cycles, until disease progression or unacceptable toxicity.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites241

Inclusion Criteria: * Women or men with histologically or cytologically confirmed carcinoma of the breast * Documented ER-positive and/or progesterone receptor-positive tumor according to American Society of Clinical Oncology/College of American Pathologists (ASCO/CAP) guidelines * Documented HER2-...

Countries:United StatesArgentinaAustraliaBrazilCanadaChinaFranceGermanyItalyJapanMexicoPolandPuerto RicoSouth AfricaSouth KoreaSpainSwitzerlandTaiwanTurkey (Türkiye)United KingdomBelgiumColombiaFinlandHong KongIndiaJordanKenyaOmanSingaporeTunisiaUgandaNew ZealandThailandDenmarkGeorgiaGreeceHungaryMalaysiaPortugalRussiaUkraine
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Competitive Landscape -Breast Cancer 402 trials

Top 20 of 92 competitors

CompanyTickerTrialsLead PhaseDrugs
AstraZeneca PLCAZN47PHASE3Fulvestrant, Capivasertib
Merck & Co., Inc.MRK12PHASE3Pembrolizumab, Paclitaxel, Doxorubicin, Epirubicin, Cyclophosphamide
Eli Lilly and CompanyLLY27PHASE3Abemaciclib, Standard Adjuvant Endocrine Therapy
BioNTech SE Sponsored ADRBNTX7PHASE3DB-1303/BNT323, T-DM1
Gilead Sciences, Inc.GILD13PHASE3Sacituzumab Govitecan-hziy, Eribulin, Capecitabine Product, Gemcitabine, Vinorelbine
Novartis AG Sponsored ADRNVS30PHASE3Ribociclib
Pfizer Inc.PFE34PHASE3ARV-471, Fulvestrant
BeOne Medicines Ltd. Sponsored ADRONC5PHASE3BGB-43395, Letrozole, Abemaciclib, Palbociclib, Ribociclib
Olema Pharmaceuticals, Inc.OLMA5PHASE3Palazestrant, Fulvestrant, Anastrozole, Letrozole, Exemestane
Jazz Pharmaceuticals Public Limited CompanyJAZZ3PHASE3Zanidatamab, Trastuzumab, Eribulin, Vinorelbine, Gemcitabine
Celcuity Inc.CELC3PHASE3Gedatolisib, Palbociclib, Fulvestrant, Alpelisib
Relay Therapeutics, Inc.RLAY2PHASE3Zovegalisib, Capivasertib, Fulvestrant
GSK plc Sponsored ADRGSK2PHASE3Niraparib
Greenwich LifeSciences, Inc.GLSI1PHASE3GLSI-100
Bristol-Myers Squibb CompanyBMY5PHASE2Iza-bren, Nab-paclitaxel, Paclitaxel, Capecitabine, Carboplatin
BriaCell Therapeutics CorpBCTX2PHASE3SV-BR-1-GM, Cyclophosphamide, Interferon infiltration of the inoculation site, Retifanlimab, Treatment of Physician's Choice
Incyte CorporationINCY4PHASE2Ruxolitinib, Capecitabine, Regorafenib
Natera, Inc.NTRA3PHASE2Discontinuation of the anti-HER2 maintenance therapy
Puma Biotechnology, Inc.PBYI3PHASE2Neratinib, Loperamide, Colesevelam
Atossa Therapeutics, Inc.ATOS1PHASE2endoxifen, goserelin
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Recent Changes (Last 90 Days)

LOWSep 3, 2026NCT06790693primaryCompletionDate: changed
LOWSep 3, 2026NCT07287150lastUpdatePostDate: changed
LOWSep 3, 2026NCT06790693primaryCompletionDate: changed
LOWSep 3, 2026NCT07287150lastUpdatePostDate: changed
LOWSep 1, 2026NCT05646862Status: ACTIVE_NOT_RECRUITING → RECRUITING
LOWSep 1, 2026NCT05646862Status: ACTIVE_NOT_RECRUITING → RECRUITING
MEDIUMAug 31, 2026NCT07054190Enrollment: 60 → 120
MEDIUMAug 31, 2026NCT07054190Enrollment: 60 → 120
LOWAug 25, 2026NCT05894239lastUpdatePostDate: changed
LOWAug 25, 2026NCT05894239lastUpdatePostDate: changed
LOWAug 20, 2026NCT06496568lastUpdatePostDate: changed
LOWAug 20, 2026NCT06496568lastUpdatePostDate: changed
LOWAug 17, 2026NCT04929223lastUpdatePostDate: changed
LOWAug 17, 2026NCT04929223lastUpdatePostDate: changed
LOWAug 11, 2026NCT07405801lastUpdatePostDate: changed
LOWAug 11, 2026NCT07405801lastUpdatePostDate: changed
LOWAug 6, 2026NCT07368998lastUpdatePostDate: changed
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LOWAug 5, 2026NCT07748208NEW_TRIAL: changed
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Frequently asked questions about Inavolisib

What is Inavolisib used for?

Inavolisib is an investigational small molecule being studied for multiple oncology indications, including metastatic breast cancer, PIK3CA-mutated cancers, HER2-positive breast cancer, metastatic castration-resistant prostate cancer, and metastatic colorectal cancer. It is currently in Phase 3 clinical development and has not been approved by the FDA.

What does Inavolisib target?

Inavolisib is a PI3K inhibitor, as indicated by its '-lisib' suffix, which places it in the PI3K target class. It is being studied in cancers with PIK3CA mutations, suggesting it targets the PI3K signaling pathway involved in tumor growth.

Who makes Inavolisib?

Inavolisib is being developed by Roche Holding AG, which trades under the ticker RHHBY. The company is conducting multiple clinical trials to evaluate the drug's safety and efficacy across various cancer types.

What phase is Inavolisib in?

Inavolisib is in Phase 3 clinical development, with an ongoing Phase 3 trial for PIK3CA-mutated HER2-positive metastatic breast cancer. It is also being studied in Phase 1 and Phase 2 trials for other indications. The drug is investigational and not yet FDA approved.

What clinical trials is Inavolisib in?

Inavolisib is being studied in eight active trials, including NCT05894239, a Phase 3 trial in PIK3CA-mutated HER2-positive metastatic breast cancer; NCT04929223, a Phase 1 trial in metastatic colorectal cancer; NCT06496568, a Phase 1 trial in PIK3CA-mutated cancers; and NCT07287150, a Phase 2 trial in metastatic castration-resistant prostate cancer.

Is Inavolisib the same as other PI3K inhibitors?

Inavolisib is a distinct investigational drug within the PI3K inhibitor class, differentiated by its specific chemical structure and ongoing clinical development. It is not known to be identical to any other approved or investigational PI3K inhibitor, and no alternative names have been established for it.

Other drugs targeting PIK3CA

Copanlisib ABBV· PHASE1 Paxalisib ADPT· PHASE2 Alpelisib AMGN· PHASE2 Copanlisib BAYRY· PHASE2 Alpelisib CELC· PHASE3 Gedatolisib CELC· PHASE3 Paxalisib JAZZ· PHASE2 Paxalisib KZIA· PHASE2 Alpelisib LLY· PHASE1 LY4064809 LLY· PHASE3 STX-478 LLY· PHASE1 Alpelisib NVS· PHASE3