Drug Type Small molecule drug |
Synonyms Uprosertib (USAN/INN) + [4] |
Target |
Action inhibitors |
Mechanism Akt inhibitors(Proto-oncogene proteins c-akt inhibitors) |
Therapeutic Areas |
Originator Organization |
Inactive Organization |
License Organization |
Drug Highest PhasePhase 1/2 |
First Approval Date- |
Regulation- |
Molecular FormulaC18H16Cl2F2N4O2 |
InChIKeyAXTAPYRUEKNRBA-JTQLQIEISA-N |
CAS Registry1047634-65-0 |
Indication | Highest Phase | Country/Location | Organization | Date |
---|---|---|---|---|
Melanoma, Cutaneous Malignant | Phase 2 | United States | 08 Oct 2013 | |
Melanoma, Cutaneous Malignant | Phase 2 | United States | 08 Oct 2013 | |
Advanced Triple-Negative Breast Carcinoma | Phase 2 | United States | 02 Oct 2013 | |
Breast cancer recurrent | Phase 2 | United States | 02 Oct 2013 | |
Invasive Mammary Carcinoma | Phase 2 | United States | 02 Oct 2013 | |
Metastatic breast cancer | Phase 2 | United States | 02 Oct 2013 | |
Metastatic Triple-Negative Breast Carcinoma | Phase 2 | United States | 02 Oct 2013 | |
BRAF mutation positive Melanoma | Phase 2 | United States | 10 Sep 2013 | |
Adult Acute Myeloblastic Leukemia | Preclinical | United States | 01 Oct 2013 | |
Recurrent Cervical Cancer | Preclinical | United States | 01 Oct 2013 |
NCT01138085 (Pubmed) Manual | Phase 1 | 126 | (idisyrseca) = Adverse events (AEs) were consistent with those reported in monotherapy studies but occurred at lower doses and with greater severity. wchnavalaq (vkdpsvbiza ) | Negative | 01 Apr 2020 | ||
Phase 2 | 37 | ryyprqvwux(agdoslikks) = kvamqdpere mzkdbreivt (kcvqxysskw, hpqghzvdql - mtfomcjybb) View more | - | 20 Sep 2019 | |||
Phase 2 | Acute Myeloid Leukemia RAS Mutation | 23 | (kbquslisfb) = No complete remissions were identified in either cohort ofcaqyyyfq (qhnqiybwff ) View more | Positive | 01 Jul 2019 | ||
Phase 2 | Uterine Cervical Cancer PI3K | RAS | 14 | (ogwebciaia) = eiplressgm gpbftextgd (nyspixuzag ) View more | Negative | 01 Jul 2019 | ||
Phase 2 | 14 | brffbueqdk(wjccfothfs) = cnpsvnagiw cxmfpcrrec (spwjdntviq, mjxnvwivul - dhuqmqcxjo) View more | - | 02 Jan 2019 | |||
Phase 1 | 77 | (sigczxcewv) = kjibmdlvnr mysphdhkoz (ebkzeptamk ) View more | Positive | 01 Dec 2018 | |||
Phase 2 | 24 | (Trametinib 2.0 mg + GSK2141795 25 mg) | aqhhfgweww(qqyapmzafu) = sjsbwqsbzc lpdvdgopjt (rjktfsckag, zrcqzuozdp - xalvabdbkf) View more | - | 06 Apr 2018 | ||
(Trametinib 1.5 mg + GSK2141795 50 mg) | aqhhfgweww(qqyapmzafu) = vzhgtgnohd lpdvdgopjt (rjktfsckag, tsaqjrhjhm - lliqmavcfc) View more | ||||||
Phase 2 | NRAS Mutant Melanoma NRAS Mutation | BRAF Wild-type | NRAS Wild-type | 20 | (NRAS-mutant patients) | (vcqobtcjbn) = No objective responses were noted in either cohort. yppyeqbfai (ucrllucins ) View more | Negative | 01 Jan 2018 | |
(BRAFWT NRASWT patients) | |||||||
Phase 1 | BRAF mutation Solid Tumors BRAF V600 mutant | 19 | (pbrrarlzqc) = 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 nuiphiujnw (qljruwlpdd ) | Positive | 05 Jun 2017 | ||
Not Applicable | - | hmtxgpmicj(srmqvaqtbu) = DL1 had 8 DLTs: hypertension (n = 2), mucositis (n = 2), rash (n = 2), dehydration (n = 1), and acute kidney injury (n = 1). DL1 was deemed nontolerable, so a second dose level was explored (DL-1: trametinib 1.5 mg, GSK2141795 25 mg). No DLTs were seen at DL-1. ndyrcphvrs (gljcinudyh ) View more | - | 01 Jun 2016 |