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Therapy Name | Trametinib + Uprosertib |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Trametinib | Mekinist | GSK1120212 | MEK inhibitor (Pan) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 | Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafinib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, and BRAF V600E-mutant anaplastic thyroid cancer (FDA.gov). |
Uprosertib | GSK2141795|GSK-2141795|GSK 2141795 | Akt Inhibitor (Pan) 19 AKT Inhibitor (Pan) - ATP competitive 7 | Uprosertib (GSK2141795) is an ATP-competitive inhibitor of AKT, which leads to inhibition of PI3K/AKT signaling potentially resulting in inhibition of cell proliferation and anti-tumor growth (PMID: 24978597, PMID: 32062691). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
Unknown unknown | endometrial cancer | no benefit | Trametinib + Uprosertib | Phase I | Actionable | In a Phase I trial, Mekinist (trametinib) and Uprosertib (GSK2141795) combination treatment demonstrated increased toxicity and limited efficacy, resulted in no response (0/14) at RP2D dose and 1 response (8.3%, 1/12) at reduced dose in patients with recurrent endometrial cancer, with progression-free survival at 6 months in 14% and 25% of the patients, respectively (PMID: 31623857). | 31623857 |
Unknown unknown | Advanced Solid Tumor | no benefit | Trametinib + Uprosertib | Phase I | Actionable | In a Phase I trial, the combination of Trametinib (GSK1120212) and Uprosertib (GSK2141795) was not well-tolerated and resulted in minimal efficacy in patients with advanced solid tumors (n=126), demonstrating an objective response rate of less than 5%, with one complete response and five partial responses (PMID: 32062691). | 32062691 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01958112 | Phase II | Trametinib + Uprosertib | GSK1120212+GSK2141795 for Cervical Cancer | Terminated | USA | 0 |
NCT01941927 | Phase II | Trametinib + Uprosertib | Trametinib With GSK2141795 in BRAF Wild-type Melanoma | Completed | USA | 0 |
NCT01907815 | Phase II | Trametinib + Uprosertib | Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Acute Myeloid Leukemia | Terminated | USA | 0 |
NCT01979523 | Phase II | Trametinib Trametinib + Uprosertib | Trametinib With or Without GSK2141795 in Treating Patients With Metastatic Uveal Melanoma | Completed | USA | 2 |
NCT01935973 | Phase II | Trametinib Trametinib + Uprosertib | Trametinib With or Without GSK2141795 in Treating Patients With Recurrent or Persistent Endometrial Cancer | Completed | USA | 0 |
NCT01989598 | Phase II | Trametinib + Uprosertib | Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Relapsed or Refractory Multiple Myeloma | Active, not recruiting | CAN | 0 |
NCT01138085 | Phase I | Trametinib + Uprosertib | Safety, Pharmacokinetics (PK) of AKT and MEK Combination | Completed | USA | 0 |
NCT01964924 | Phase II | Trametinib + Uprosertib | Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Metastatic Triple-Negative Breast Cancer | Completed | USA | 0 |