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GDC-0941

Phase 2

Breast Cancer | Small molecule | Oncology |Roche Holding AG|Last Updated: Apr 24, 2017

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials2
Total Enrollment501

FDA Designations

No designations recorded

Clinical trial landscape

GDC-0941 · 11 trials · 8 indications

Phase 2 2Phase 1 9
NCT01740336A Study of Paclitaxel With GDC-0941 Versus Paclitaxel With Placebo in Participants With Locally Recurrent or Metastatic Breast CancerBreast Cancer
COMPLETED183 Analytics
NCT01437566Study of GDC-0941 or GDC-0980 With Fulvestrant Versus Fulvestrant in Advanced or Metastatic Breast Cancer in Participants Resistant to Aromatase Inhibitor TherapyBreast Cancer
COMPLETED318 Analytics
PHASE2COMPLETED
A Study of Paclitaxel With GDC-0941 Versus Paclitaxel With Placebo in Participants With Locally Recurrent or Metastatic Breast Cancer
Breast CancerUnlock trial analytics
PHASE2COMPLETED
Study of GDC-0941 or GDC-0980 With Fulvestrant Versus Fulvestrant in Advanced or Metastatic Breast Cancer in Participants Resistant to Aromatase Inhibitor Therapy
Breast CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression-Free Survival (PFS) Assessed as per Modified Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.1 (v1.1)
From the time of randomization until disease progression or death from any cause (up to approximately 3 years)
Progression Free Survival as Assessed by the Investigator Per modified RECIST v 1.1
From Screening to up to approximately 5 years (assessed at Screening, after 8, 16, 24 and 32 weeks of treatment, every 12 weeks thereafter until disease progression or initiation of other anti-cancer therapy)
Percentage of Participants with Adverse Events
Baseline to up to 30 days after the last dose of study drug (Approximately 5 years)
Area under the concentration-time curve (AUC) of plasma GDC-0941
25 Days
Maximum plasma concentration (Cmax) of GDC-0941
25 Days
Relative bioavailability (Frel) according to the model independent approach
25 days
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal elimination half-life
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent terminal phase elimination rate constant
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent total clearance
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: apparent volume of distribution
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve extrapolated to infinity
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: area under the concentration-time curve from Hour 0 to the last measurable concentration
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: maximum observed concentration
up to approximately 6 weeks or early study discontinuation
Pharmacokinetic property based on the plasma concentrations of total radioactivity and GDC-0941: time to maximum concentration
up to approximately 6 weeks or early study discontinuation
Incidence, nature, and severity of adverse events
Through study completion or early study discontinuation
Pharmacokinetic parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration)
Prior to and after GDC-0941 dosing
PK parameters of GDC-0941 (total exposure, maximum and minimum plasma concentration)
Following administration of study drug
Number of Participants with Dose Limiting Toxicities (DLTs)
Days 1 to 22 of Cycle 1
Percentage of Participants with Adverse Events (AEs)
Up to approximately 5.5 years
Tumor response
Assessed at periodic intervals
Changes in cardiac function
Through study completion or early study discontinuation
Changes in vital signs, physical findings, and clinical laboratory results during and following administration of study drugs that result in dose modification, dose delay, or discontinuation of T-DM1 and/or GDC 0941
Through study completion or early study discontinuation
Occurrence of adverse events by NCI CTCAE grade and associated dose of GDC-0941
Through study completion or early study discontinuation
Occurrence of dose-limiting toxicities (DLTs) by NCI CTCAE grade and associated dose of GDC-0941
Through study completion or early study discontinuation
Occurrence of Grade 3 or 4 abnormalities in safety-related laboratory parameters and associated dose of GDC-0941
Through study completion or early study discontinuation
PK parameters after single and multiple doses of GDC-0941
Through study completion or early study discontinuation
Maximum Observed Concentration (Cmax) of GDC-0941
Pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24, 48, 72 h) Day 1; pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24 h) Days 8 and 15; pre-dose (5 min) Days 22, 29, 36, and end of Cycles 1 to 12 (up to 1 year overall)
Terminal Elimination Half-Life (t1/2) of GDC-0941
Pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24, 48, 72 h) Day 1; pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24 h) Days 8 and 15; pre-dose (5 min) Days 22, 29, 36, and end of Cycles 1 to 12 (up to 1 year overall)
Area Under the Concentration-Time Curve (AUC) of GDC-0941
Pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24, 48, 72 h) Day 1; pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24 h) Days 8 and 15; pre-dose (5 min) Days 22, 29, 36, and end of Cycles 1 to 12 (up to 1 year overall)
Percentage of Participants with Dose-Limiting Toxicities (DLTs)
Visits during treatment on Days 1, 2, 3, 4, 8, 15, 22, 29, 36
Percentage of Participants with Grade 3 or 4 Abnormalities in Safety-Related Laboratory Parameters
Visits at Baseline and during treatment on Days 1, 8, 15, 22, 29, 36; weekly during Cycle 2; every two weeks during Cycles 3 to 6; every month during Cycles 7 to 12; and up to 30 days after last dose (up to 1 year overall)
Time of Maximum Observed Concentration (Tmax) of GDC-0941
Pre-dose (5 minutes [min]) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24, 48, 72 hours [h]) Day 1; pre-dose (5 min) and post-dose (0.5, 1, 2, 3, 4, 8, 12, 24 h) Days 8 and 15; pre-dose (5 min) Days 22, 29, 36, and end of Cycles 1 to 12 (up to 1 year overall)

Secondary Endpoints

Percentage of Participants With Adverse Events
From randomization up to approximately 3 years
Percentage of Participants With Objective Tumor Response Assessed as per Modified RECIST v1.1
From first observation of an objective tumor response until disease progression (up to approximately 3 years)
Percentage of Participants Acheiving Clinical Benefit (Partial Response, Complete Response or Stable Disease Lasting for at Least 6 Months) Assessed as per Modified RECIST v1.1
From randomization until disease progression (up to approximately 3 years)
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Study Design & Arms

AllocationRANDOMIZED
MaskingSINGLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
A: Paclitaxel, GDC-0941EXPERIMENTALParticipants will receive GDC-091 260 milligrams (mg) orally in repeated rounds of once daily (QD) dosing for 5 consecutive days followed by 2 consecutive days during which GDC-0941 will not be administered (5/7-day schedule). This 5/7-day schedule will be repeated weekly in each 28-day cycle until disease progression or intolerable toxicity. Participants will receive 90 milligrams per square meter (mg/m\^2) intravenously (IV) weekly for 3 out of 4 weeks in every 28-day cycle.
B: Paclitaxel, PlaceboPLACEBO_COMPARATORParticipants will receive placebo matching to GDC-0941 on the 5/7-day schedule along with 90 mg/m\^2 IV weekly for 3 out of 4 weeks in every 28-day cycle.
GDC-0941 Matching Placebo + Fulvestrant (Arm E)PLACEBO_COMPARATORParticipants with PIK3CA mutation will receive fulvestrant 500 mg as 2 IM injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle and GDC-0941 matching placebo QD orally starting on Day 1 of Cycle 1, each cycle of 28 days. Study treatment will continue until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0941-260 mg + Fulvestrant (Arm D)EXPERIMENTALParticipants with PIK3CA mutation will receive fulvestrant 500 mg as 2 IM injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle and GDC-0941 260 mg QD orally starting on Day 1 of Cycle 1, each cycle of 28 days. Study treatment will continue until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0941-340 mg + Fulvestrant (Arm A)EXPERIMENTALParticipants will receive fulvestrant 500 milligrams (mg) as 2 intramuscular (IM) injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle and GDC-0941 340 mg once daily (QD) orally starting on Day 15 of Cycle 1, each cycle of 28 days. Study treatment will continue until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0948 or GDC-0980 Matching Placebo + Fulvestrant (Arm C)PLACEBO_COMPARATORParticipants will be randomized in 1:1 ratio to receive GDC-0948 matching placebo or GDC-0980 matching placebo with fulvestrant. Participants will receive fulvestrant 500 mg as 2 IM injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle and GDC-0948 or GDC-0980 matching placebo QD orally starting on Day 15 of Cycle 1, each cycle of 28 days. Study treatment will continue until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0980-30 mg + Fulvestrant (Arm B)EXPERIMENTALParticipants will receive fulvestrant 500 mg as 2 IM injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle and GDC-0980 30 mg QD orally starting on Day 15 of Cycle 1, each cycle of 28 days. Study treatment will continue until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
Crossover sequence 1EXPERIMENTAL -
Crossover sequence 2EXPERIMENTAL -
Crossover sequence 3EXPERIMENTAL -
Crossover sequence 4EXPERIMENTAL -
AEXPERIMENTALExperimental
BEXPERIMENTAL -
Part 1EXPERIMENTAL -
Part 2EXPERIMENTAL -
GDC-0941+Paclitaxel+CarboplatinEXPERIMENTALBevacizumab-ineligible non-small cell lung cancer (NSCLC) participants may receive up to 6 cycles (21-day cycle) of combination chemotherapy with paclitaxel and carboplatin along with GDC-0941
GDC-0941+Paclitaxel+Carboplatin+BevacizumabEXPERIMENTALBevacizumab-eligible NSCLC particpants may receive up to 6 cycles of combination chemotherapy with paclitaxel and carboplatin along with GDC-0941 and bevacizumab.
GDC-0941+Pemetrexed+CisplatinEXPERIMENTALBevacizumab-ineligible NSCLC participants may receive up to 6 cycles of combination chemotherapy with pemetrexed and cisplatin along with GDC-0941.\\n
GDC-0941+Pemetrexed+Cisplatin+BevacizumabEXPERIMENTALBevacizumab-eligible NSCLC participants may receive up to 6 cycles of combination chemotherapy with pemetrexed and cisplatin along with GDC-0941 and bevacizumab.\\n
CEXPERIMENTAL -
1EXPERIMENTAL -
Group A: GDC-0941 QD Dose EscalationEXPERIMENTALParticipants will receive GDC-0941 for up to 1 year, administered orally QD at a starting dose of 15 milligrams (mg).
Group B: GDC-0941 BID Dose EscalationEXPERIMENTALParticipants will receive GDC-0941 for up to 1 year, administered orally BID at a starting dose determined from Group A assessments.
Group C: GDC-0941 QD or BID ExpansionEXPERIMENTALParticipants will receive GDC-0941 for up to 1 year, administered orally QD or BID. The dose/regimen will be determined on the basis of data from Groups A and B.

Interventions

NameTypeDescription
GDC-0941DRUGGDC-0941 will be administered QD orally for 5 consecutive days each week.
PlaceboDRUGPlacebo matching to GDC-0941
PaclitaxelDRUGPaclitaxel will be administered IV weekly for 3 out of 4 weeks in every 28-day cycle.
FulvestrantDRUGParticipants will receive fulvestrant 500 mg as 2 IM injections of 250 mg on Days 1 and 15 of Cycle 1 and on Day 1 of each subsequent cycle, each cycle of 28 days until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0941 Matching PlaceboDRUGParticipants will receive GDC-0941 matching placebo QD orally from Day 1 or Day 15 of Cycle 1 until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0980DRUGParticipants will receive GDC-0980 30 mg (Part I) QD orally from Day 15 of Cycle 1 until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
GDC-0980 Matching PlaceboDRUGParticipants will receive GDC-0980 matching placebo QD orally from Day 15 of Cycle 1 until disease progression, intolerable toxicity, elective withdrawal from the study, study completion or termination.
ketoconazoleDRUGOral repeating dose
rabeprazoleDRUGOral repeating dose
bevacizumabDRUGBevacizumab 15 milligrams per kilograms (mg/kg) intravenously (IV) on Day 1 of every 3-week cycle.
carboplatinDRUGCarboplation IV on Day 1 of every 3-week cycle, at a dose to achieve an area under concentration time curve of 6 milligrams per milliliter\*minute (mg/mL\*min).\\n
cisplatinDRUGCisplatin 75 milligrams per square meter (mg/m\^2) IV on Day 1 of every 3-week cycle.\\n
pemetrexedDRUGPemetrexed 500 mg/m\^2 IV on Day 1 of every 3-week cycle.
erlotinib HClDRUGOral repeating dose
TrastuzumabDRUGIntravenous repeating dose
trastuzumab-MCC-DM1DRUGIntravenous repeating dose
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Eligibility Criteria

Age Range18 Years to N/A
SexFEMALE
Healthy VolunteersNo
Study Sites97

Inclusion Criteria: * Histologically or cytologically confirmed adenocarcinoma of the breast, with measurable or non-measurable locally recurrent or metastatic disease * Human epidermal growth factor receptor 2 (HER2)-negative and hormone receptor (HR) (estrogen receptor and/or progesterone recepto...

Countries:United StatesAustraliaAustriaBelgiumCzechiaSouth KoreaSpainUnited KingdomArgentinaCanadaChileDenmarkFranceGermanyHong KongIsraelItalyMalaysiaMexicoNew ZealandPeruRussiaSingaporeThailandNetherlands
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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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Frequently asked questions about GDC-0941

What is GDC-0941 used for?

GDC-0941, also known as pictilisib, is an investigational small molecule being studied for use in oncology. It has been evaluated in clinical trials for conditions including HER2-positive metastatic breast cancer, non-Hodgkin's lymphoma, solid cancers, non-squamous non-small cell lung cancer, and breast cancer. It is not approved and remains in clinical development.

What does GDC-0941 target?

GDC-0941 is a small molecule that targets phosphoinositide 3-kinase (PI3K). It is being investigated as a treatment for various cancers, including HER2-positive metastatic breast cancer. The drug is designed to inhibit PI3K, which plays a role in cancer cell growth and survival.

Who makes GDC-0941?

GDC-0941 is being developed by Roche Holding AG, which trades under the ticker RHHBY. The drug is also known as pictilisib. Roche is conducting clinical trials to evaluate its safety and efficacy in oncology indications.

What phase is GDC-0941 in?

GDC-0941 is in Phase 2 clinical development. It is an investigational drug and has not been approved by regulatory authorities. The clinical trials for GDC-0941 are completed, with no active trials currently listed.

What clinical trials is GDC-0941 in?

GDC-0941 has been studied in several completed clinical trials. These include NCT00928330, a Phase 1 study in HER2-positive metastatic breast cancer; NCT01240226, a bioavailability study in healthy volunteers; NCT01474668, an absorption, metabolism, and excretion study; and NCT02092831, a formulation study in healthy volunteers.

Is GDC-0941 the same as pictilisib?

Yes, GDC-0941 is also known as pictilisib. The drug is being developed by Roche Holding AG for oncology indications. Clinical trials have used both names to refer to the same investigational small molecule.