Therapy Detail

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Therapy Name Trametinib + Uprosertib
Synonyms
Therapy Description

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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) 18 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).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

Sorting

  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

Sorting

  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

Clinical Trial Phase Therapies Title Recruitment Status
NCT01138085 Phase I Trametinib + Uprosertib Safety, Pharmacokinetics (PK) of AKT and MEK Combination Completed
NCT01964924 Phase II Trametinib + Uprosertib Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Metastatic Triple-Negative Breast Cancer Completed
NCT01941927 Phase II Trametinib + Uprosertib Trametinib With GSK2141795 in BRAF Wild-type Melanoma Completed
NCT01935973 Phase II Trametinib Trametinib + Uprosertib Trametinib With or Without GSK2141795 in Treating Patients With Recurrent or Persistent Endometrial Cancer Active, not recruiting
NCT01958112 Phase II Trametinib + Uprosertib GSK1120212+GSK2141795 for Cervical Cancer Terminated
NCT01989598 Phase II Trametinib + Uprosertib Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Relapsed or Refractory Multiple Myeloma Active, not recruiting
NCT01979523 Phase II Trametinib Trametinib + Uprosertib Trametinib With or Without GSK2141795 in Treating Patients With Metastatic Uveal Melanoma Completed
NCT01907815 Phase II Trametinib + Uprosertib Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Acute Myeloid Leukemia Terminated


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