Clinical Trials

Taselisib has been evaluated in multiple Phase I, Phase II, and Phase III clinical trials targeting advanced solid tumors, squamous cell lung carcinoma, breast cancer subtypes, and pharmacokinetic profiles in healthy volunteers. These studies have been sponsored by major pharmaceutical entities like Genentech and Hoffmann-La Roche, alongside cooperative networks such as the National Cancer Institute and SWOG Cancer Research Network. Protocol recruitment statuses encompass completed, active not recruiting, and terminated outcomes, notably across Phase II lung cancer and Phase III breast cancer evaluations.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02465060 ACTIVE_NOT_RECRUITING
Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Bladder Carcinoma; Breast Carcinoma; Cervical Carcinoma; Colon Carcinoma; Colorectal Carcinoma; Endometrial Carcinoma; Esophageal Carcinoma; Exocrine Pancreas Carcinoma; Gastric Carcinoma; Glioma; Head and Neck Carcinoma; Hematopoietic and Lymphoid Cell Neoplasm; Kidney Carcinoma; Liver Carcinoma; Lung Carcinoma; Lymphoma; Malignant Uterine Corpus Neoplasm; Malignant Uterine Neoplasm; Melanoma; Multiple Myeloma; Ovarian Carcinoma; Prostate Carcinoma; Rectal Carcinoma; Recurrent Bladder Carcinoma; Recurrent Breast Carcinoma; Recurrent Cervical Carcinoma; Recurrent Colon Carcinoma; Recurrent Colorectal Carcinoma; Recurrent Esophageal Carcinoma; Recurrent Gastric Carcinoma; Recurrent Glioma; Recurrent Head and Neck Carcinoma; Recurrent Liver Carcinoma; Recurrent Lung Carcinoma; Recurrent Lymphoma; Recurrent Malignant Solid Neoplasm; Recurrent Malignant Uterine Corpus Neoplasm; Recurrent Melanoma; Recurrent Multiple Myeloma; Recurrent Ovarian Carcinoma; Recurrent Pancreatic Carcinoma; Recurrent Prostate Carcinoma; Recurrent Rectal Carcinoma; Recurrent Skin Carcinoma; Recurrent Thyroid Gland Carcinoma; Refractory Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Multiple Myeloma; Skin Carcinoma; Thyroid Gland Carcinoma
National Cancer Institute (NCI)
 2015-08-17 PHASE2
NCT02390427 COMPLETED
Metastatic Breast Cancer; Recurrent Breast Cancer
Otto Metzger, MD
 2015-04-20 PHASE1
NCT02340221 TERMINATED
Breast Cancer
Hoffmann-La Roche
 2015-04-09 PHASE3
NCT04439175 ACTIVE_NOT_RECRUITING
Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Hematopoietic and Lymphoid Cell Neoplasm; Refractory Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Multiple Myeloma
National Cancer Institute (NCI)
 2016-02-25 PHASE2
NCT03290092 TERMINATED
PIK3CA-Related Overgrowth
Centre Hospitalier Universitaire Dijon
 2017-07-31 PHASE1; PHASE2
NCT02457910 TERMINATED
Estrogen Receptor Negative; Estrogen Receptor Positive; HER2/Neu Negative; Progesterone Receptor Negative; Progesterone Receptor Positive; Stage IV Breast Cancer; Triple-Negative Breast Carcinoma
Vanderbilt-Ingram Cancer Center
 2015-06 PHASE1; PHASE2
NCT02389842 COMPLETED
Advanced Solid Tumours; Breast Cancer
Royal Marsden NHS Foundation Trust
 2015-03-25 PHASE1
NCT02273973 COMPLETED
Breast Cancer
Genentech, Inc.
 2014-11-12 PHASE2
NCT02785913 COMPLETED
Recurrent Squamous Cell Lung Carcinoma; Stage IV Squamous Cell Lung Carcinoma
SWOG Cancer Research Network
 2014-11 PHASE2
NCT02785913 Completed
Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma
SWOG Cancer Research Network|National Cancer Institute (NCI)
 2014-11 Phase 2
NCT01967966 Completed
Healthy Volunteer
Genentech Inc.
 2013-11 Phase 1
NCT01814709 Completed
Healthy Volunteer
Genentech Inc.
 2013-04 Phase 1

(data from https://clinicaltrials.gov, updated on 2026-08-28)

Check the Taselisib (GDC 0032) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Taselisib is a potent, β-isoform-sparing phosphatidylinositol 3-kinase inhibitor that selectively binds the alpha, delta, and gamma isoforms of PI3K. By potently blocking PI3K enzymatic activity, taselisib disrupts downstream signaling through the AKT pathway, leading to suppressed cell growth and impaired cell survival. Consequently, this inhibition restricts tumor proliferation and induces apoptosis, providing a mechanistic basis for its investigation in clinical trials targeting advanced solid tumors, breast cancer, and squamous cell lung 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.