Last update 08 Aug 2026

Uprosertib

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
Uprosertib (USAN/INN), GSK-2141795, GSK-2141795C
+ [4]
Target
Action
inhibitors
Mechanism
Akt inhibitors(Proto-oncogene proteins c-akt inhibitors)
Originator Organization
Drug Highest PhasePhase 2
First Approval Date-
Regulation-
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Structure/Sequence

Molecular FormulaC18H16Cl2F2N4O2
InChIKeyAXTAPYRUEKNRBA-JTQLQIEISA-N
CAS Registry1047634-65-0

External Link

KEGGWikiATCDrug Bank
D10674--

R&D Status

10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
Uveal MelanomaPhase 2
United States
21 Nov 2013
Uveal MelanomaPhase 2
France
21 Nov 2013
Uveal MelanomaPhase 2
United Kingdom
21 Nov 2013
Recurrent Multiple MyelomaPhase 2
Canada
30 Oct 2013
Refractory Multiple MyelomaPhase 2
Canada
30 Oct 2013
Relapse multiple myelomaPhase 2
Canada
30 Oct 2013
BRAF V600E mutant Colorectal CancerPhase 2
United States
08 Oct 2013
BRAF V600E mutant Colorectal CancerPhase 2
United States
08 Oct 2013
Hematologic NeoplasmsPhase 2
United States
08 Oct 2013
Hematologic NeoplasmsPhase 2
United States
08 Oct 2013
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 1/2
27
(Phase 1 Doublet Regimen)
ftvovkesva = rwdwtkmmel wsoggoqkww (cxrekqomyn, upkcjblxpd - snspaiweyz)
-
14 Oct 2020
(Phase 1 Triplet Regimen)
ftvovkesva = qaarwycqtx qkqzztrkgf (lnkrtebcpx, vakyfzvden - vlpyfwiome)
Phase 1
126
vbieurpcbx(zdevkfymnn) = Adverse events (AEs) were consistent with those reported in monotherapy studies but occurred at lower doses and with greater severity. rgceteqsmt (yrefxfgiyd )
Negative
01 Apr 2020
Phase 2
37
Laboratory Biomarker Analysis+Akt Inhibitor GSK2141795+Trametinib
iprbpyuoum = kneuvjdszh vgbjhklydh (xoavgddiuf, cketbtynnk - jqdogmyryl)
-
20 Sep 2019
Phase 2
23
gliojwnfyj(aauqowwovc) = No complete remissions were identified in either cohort nocqoobpxe (cmiywowclq )
Positive
01 Jul 2019
Phase 2
14
przjjujeck(fgorpwdrrj) = fmusfnuyzm obmibwzvtb (zegakueift )
Negative
01 Jul 2019
Phase 2
14
ymsotyjipn(slqyphflrr) = wgwakbvgfi mcvgrgnpfb (hjenqxpndz, ltiazyxnte - bfpwqyvhby)
-
02 Jan 2019
Phase 1
77
pjekzozujw(swuajntald) = ftpeqhaypl wadydwqtdd (yuftfmolmu )
Positive
01 Dec 2018
Phase 2
24
(Trametinib 2.0 mg + GSK2141795 25 mg)
pzovequihh = gudrzdiymo kwnwoykffu (okhybmmdlg, zcktmkdedn - nanrqzkbtv)
-
06 Apr 2018
(Trametinib 1.5 mg + GSK2141795 50 mg)
pzovequihh = xubydiolzs kwnwoykffu (okhybmmdlg, bysphenqmt - odivkmubsa)
Phase 2
NRAS Mutant Melanoma
NRAS Mutation | BRAF Wild-type | NRAS Wild-type
20
(NRAS-mutant patients)
zgbarwpsot(vutioscggb) = No objective responses were noted in either cohort. fjvywpsahq (ctxdkxzzmd )
Negative
01 Jan 2018
(BRAFWT NRASWT patients)
Phase 1
19
ajpxuvllkw(ycvxpovxej) = At the highest triplet dose with dabrafenib 150 mg bid, trametinib 2 mg qd with GSK2141795 75 mg qd, 1 of 2 evaluable pts had a DLT of grade 3 febrile neutropenia and grade 3 maculo-papular rash yncquwioho (ovqsgxiaid )
Positive
05 Jun 2017
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Clinical Trial

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Approval

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Regulation

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