Clinical Trials

Uprosertib (GSK2141795) has been evaluated in multiple Phase 1 and Phase 2 clinical trials across various oncology indications, including advanced solid tumors, melanoma, cervical cancer, endometrial adenocarcinoma, triple-negative breast carcinoma, and plasma cell myeloma. Sponsored by pharmaceutical entities, government bodies, and academic institutions, these studies assessed uprosertib as a monotherapy or in combination regimens, such as with MEK inhibitors. Overall recruitment statuses for these investigations include completed, active not recruiting, and terminated.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01989598 COMPLETED
Recurrent Plasma Cell Myeloma; Refractory Plasma Cell Myeloma
National Cancer Institute (NCI)
 2013-10-30 PHASE2
NCT01902173 COMPLETED
Hematopoietic and Lymphoid Cell Neoplasm; Locally Advanced Malignant Solid Neoplasm; Locally Advanced Melanoma; Metastatic Malignant Solid Neoplasm; Metastatic Melanoma; Stage IIIC Cutaneous Melanoma AJCC v7; Stage IV Cutaneous Melanoma AJCC v6 and v7; Unresectable Malignant Solid Neoplasm; Unresectable Melanoma
National Cancer Institute (NCI)
 2013-10-08 PHASE1; PHASE2
NCT01958112 TERMINATED
Cervical Cancer
Dana-Farber Cancer Institute
 2013-10 PHASE2
NCT01979523 ACTIVE_NOT_RECRUITING
Recurrent Uveal Melanoma; Stage IV Uveal Melanoma AJCC v7
National Cancer Institute (NCI)
 2013-11-21 PHASE2
NCT01964924 COMPLETED
Estrogen Receptor Negative; HER2/Neu Negative; Invasive Breast Carcinoma; Progesterone Receptor Negative; Recurrent Breast Carcinoma; Stage IV Breast Cancer; Triple-Negative Breast Carcinoma
National Cancer Institute (NCI)
 2013-10-02 PHASE2
NCT01907815 TERMINATED
Recurrent Adult Acute Myeloid Leukemia; Untreated Adult Acute Myeloid Leukemia
National Cancer Institute (NCI)
 2013-10 PHASE2
NCT01935973 COMPLETED
Endometrial Adenocarcinoma; Endometrial Clear Cell Adenocarcinoma; Endometrial Mixed Cell Adenocarcinoma; Endometrial Serous Adenocarcinoma; Endometrial Undifferentiated Carcinoma; Recurrent Uterine Corpus Cancer
National Cancer Institute (NCI)
 2013-09-30 PHASE1
NCT01138085 COMPLETED
Cancer
GlaxoSmithKline
 2010-05-04 PHASE1
NCT01941927 COMPLETED
Melanoma
Adil Daud
 2013-09-10 PHASE2
NCT01958112 Terminated
Cervical Cancer
Dana-Farber Cancer Institute|Novartis|National Comprehensive Cancer Network
 2013-10 Phase 2
NCT01941927 Completed
Melanoma
Adil Daud|National Comprehensive Cancer Network|University of California San Francisco
 2013-09-10 Phase 2
NCT00920257 COMPLETED
Cancer
GlaxoSmithKline
 2009-06-16 PHASE1
NCT01266954 COMPLETED
Solid Tumours
GlaxoSmithKline
 2010-06-01 PHASE1
NCT01266954 Completed
Solid Tumours
GlaxoSmithKline
 2010-06-01 Phase 1
NCT01138085 Completed
Cancer
GlaxoSmithKline
 2010-05-04 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-03-02)

Check the Uprosertib (GSK2141795) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Uprosertib is a selective, ATP-competitive pan-Akt kinase inhibitor that potently binds to Akt isoforms 1, 2, and 3, thereby blocking downstream serine/threonine phosphorylation and impairing key oncogenic survival signaling pathways. By inhibiting Akt-mediated cellular proliferation and inducing apoptotic signaling, uprosertib suppresses tumor cell growth and survival, demonstrating therapeutic relevance across evaluated clinical conditions such as melanoma, cervical cancer, and solid tumors.

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.