Therapy Detail

Therapy Name ABT-263 + Alpelisib + CGM097 + Trametinib
Therapy Description


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Drug Name Trade Name Synonyms Drug Classes Drug Description
Alpelisib BYL719 PIK3CA inhibitor 14 Alpelisib (BYL719) is a selective PIK3CA inhibitor that blocks activation of the PI3K signaling pathway and inhibits tumor growth (PMID: 23726034).
CGM097 NVP-CGM097 MDM2 Inhibitor 17 CGM097 binds to the p53 binding region of MDM2 and prevents MDM2-p53 interaction, resulting in activation of p53 signaling and decreased tumor growth (Cancer Res October 1, 2014 74:4638).
Navitoclax ABT-263 BCL-XL inhibitor 9 BCL2 inhibitor 15 Navitoclax (ABT-263) is a BCL2, BCL-XL, and BCL-W inhibitor, which may enhance the efficacy of chemotherapeutics (PMID: 25787766).
Trametinib Mekinist GSK1120212 MEK inhibitor (Pan) 20 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 (
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KRAS mut + TP53 wild-type colorectal cancer sensitive ABT-263 + Alpelisib + CGM097 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of Navitoclax (ABT-263), Alpelisib (BYL719), Mekinist (trametinib), and CGM097 resulted in the greatest synergistic effect and inhibition of cell growth in colorectal cancer cells harboring a KRAS mutation and wild-type TP53 in culture compared to the double or triple combinations of the therapies (PMID: 27659046). 27659046
Clinical Trial Phase Therapies Title Recruitment Status