Clinical Trials

Multiple Phase 1 and Phase 2 clinical trials sponsored by Genentech, Inc. have evaluated the safety, pharmacokinetics, and therapeutic efficacy of apitolisib (GDC-0980), all of which have completed recruitment. These studies assessed the compound as monotherapy or in combination regimens across several indications, including advanced solid tumors, breast cancer, castration-resistant prostate cancer, endometrial carcinoma, metastatic renal cell carcinoma, and non-Hodgkin's lymphoma, alongside pharmacokinetic evaluations in healthy volunteers.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01437566 COMPLETED
Breast Cancer
Genentech, Inc.
 2011-10 PHASE2
NCT01485861 COMPLETED
Prostate Cancer
Genentech, Inc.
 2012-01-11 PHASE1; PHASE2
NCT01332604 COMPLETED
Solid Cancers
Genentech, Inc.
 2011-07 PHASE1
NCT00854152 COMPLETED
Non-Hodgkin's Lymphoma, Solid Cancers
Genentech, Inc.
 2009-03 PHASE1
NCT01301716 COMPLETED
Solid Cancers
Genentech, Inc.
 2011-09 PHASE1
NCT01442090 COMPLETED
Renal Cell Carcinoma
Genentech, Inc.
 2011-10 PHASE2
NCT01455493 COMPLETED
Endometrial Carcinoma
Genentech, Inc.
 2011-12 PHASE2
NCT01254526 COMPLETED
Breast Cancer
Genentech, Inc.
 2010-12 PHASE1
NCT00854126 COMPLETED
Non-Hodgkin's Lymphoma, Solid Cancers
Genentech, Inc.
 2009-05 PHASE1
NCT01487239 COMPLETED
Healthy Volunteer
Genentech, Inc.
 2011-12 PHASE1
NCT01487239 Completed
Healthy Volunteer
Genentech Inc.
 2011-12 Phase 1
NCT01455493 Completed
Endometrial Carcinoma
Genentech Inc.
 2011-12 Phase 2
NCT01473316 COMPLETED
Healthy Volunteer
Genentech, Inc.
 2011-11 PHASE1
NCT01442090 Completed
Renal Cell Carcinoma
Genentech Inc.
 2011-10 Phase 2
NCT01287091 COMPLETED
Healthy Volunteer
Genentech, Inc.
 2010-10-14 PHASE1
NCT01254526 Completed
Breast Cancer
Genentech Inc.
 2010-12 Phase 1
NCT00854126 Completed
Non-Hodgkin''s Lymphoma Solid Cancers
Genentech Inc.
 2009-05 Phase 1
NCT00854152 Completed
Non-Hodgkin''s Lymphoma Solid Cancers
Genentech Inc.
 2009-03 Phase 1

(data from https://clinicaltrials.gov, updated on 2016-11-02)

Check the Apitolisib (GDC-0980) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Apitolisib (GDC-0980) acts as a potent, dual ATP-competitive inhibitor of class I PI3K isoforms and mTOR kinase, thereby suppressing downstream Akt phosphorylation and signal transduction across the PI3K/Akt/mTOR pathway. This dual enzymatic blockade induces G1-phase cell cycle arrest, triggers apoptosis, and stimulates autophagy, driving tumor growth suppression in pathway-activated malignancies such as renal cell carcinoma, breast cancer, and endometrial carcinoma.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.