Therapy Detail

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Therapy Name MK2206
Synonyms
Therapy Description

MK2206 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway and tumor cell proliferation (PMID: 20571069).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
MK2206 MK-2206 Akt Inhibitor (Pan) 20 MK2206 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway and tumor cell proliferation (PMID: 20571069, PMID: 32194695).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA H1047R thyroid gland cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an anaplastic thyroid cancer cell line harboring PIK3CA H1047R (PMID: 21289267). 21289267
PIK3CA E542K stomach cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a gastric cancer cell line harboring PIK3CA E542K in culture (PMID: 32439931). 32439931
NRAS Q61R thyroid gland cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an anaplastic thyroid cancer cell line harboring NRAS Q61R (PMID: 21289267). 21289267
PIK3CA G1049R breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA H1047R breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
PIK3CA H1047R breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA E542K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). 26627007
PTEN R130* thyroid gland follicular carcinoma sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an follicular thyroid cancer cell line harboring PTEN R130* and loss of one PTEN allele (PMID: 21289267). 21289267
PIK3CA mutant endometrial cancer no benefit MK2206 Phase II Actionable In a Phase II trial, MK2226 demonstrated limited benefit in endometrial cancer patients regardless of PIK3CA status, with partial responses in 6% (2/37) of patients, 19% (7/37; 5 with serous histology) remaining progression-free for at least 6 mo, and a median progression-free survival (PFS) of 2.0 mo in the overall population, and partial responses in 11% (11/9), 33% (3/9) progression-free for 6 mo, and a median PFS of 1.7 mo in the group of patients with PIK3CA mutations (PMID: 31714586; NCT01307631). 31714586
PIK3CA P449T colorectal cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a colorectal cancer cell line harboring PIK3CA P449T in culture (PMID: 32439931). 32439931
PTEN loss prostate cancer no benefit MK2206 Phase I Actionable In a Phase I clinical trial, 8 patients with metastatic, castration-resistant prostate cancer harboring a loss of PTEN did not respond to MK-2206 therapy, but prolonged stable disease was observed in 2 patients (PMID: 26187616). 26187616
PIK3CA N345K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA E545K breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment inhibited Akt signaling, induced cell death, and inhibited proliferation of breast cancer cell lines harboring PIK3CA E545K in culture (PMID: 32439931). 32439931
PIK3CA E545K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PTEN L108R breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 32439931). 32439931
PTEN L108R breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK-2206 inhibited proliferation of a breast cancer cell line harboring PTEN L108R in culture (PMID: 30858154). 30858154
PIK3CA E542K thyroid gland papillary carcinoma sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including a papillary thyroid cancer cell line harboring PIK3CA E542K (PMID: 21289267). 21289267
PIK3CA amp nasopharynx carcinoma sensitive MK2206 Phase II Actionable In a Phase II study, MK2206 increased stable disease to 12 months in a nasopharyngeal carcinoma patient with Pik3ca amplification (PMID: 26084990). 26084990
PIK3CA E545K thyroid gland cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, expression of PIK3CA E545K in a thyroid cancer cell line resulted in increased sensitivity to MK2206 in culture (PMID: 21289267). 21289267
PIK3CA mutant breast cancer no benefit MK2206 Phase II Actionable In a Phase II trial, MK2206 demonstrated limited clinical efficacy in patients with advanced breast cancer harboring mutations in PIK3CA (n=14) or AKT1 (n=4), resulted in an objective response rate of 5.6% (1/18, 1 partial response) and a 6-month progression-free survival rate of 5.6%, with no significant target inhibition in tumor biopsies (PMID: 31277699; NCT01277757). 31277699
PTEN loss osteosarcoma sensitive MK2206 Preclinical - Pdx Actionable In a preclinical study, a patient derived xenograft (PDX) model of osteosarcoma with biallelic loss of PTEN was sensitive to treatment with MK2206, demonstrating reduced tumor growth and increased apoptotic activity (PMID: 30266815). 30266815
PIK3CA act mut breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, breast cancer cell lines harboring activating mutations in PIK3CA had increased sensitivity to MK2206 in cell culture (PMID: 22932669). 22932669
HRAS G13R thyroid gland cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an anaplastic thyroid cancer cell line harboring HRAS G13R (PMID: 21289267). 21289267
MAP2K1 L98_K104delinsQ Advanced Solid Tumor resistant MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment failed to inhibit activation of Mek and Erk in human cells expressing MAP2K1 L98_K104delinsQ in culture (PMID: 29768711). 29768711
PIK3CA K111N breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PTEN loss breast cancer no benefit MK2206 Phase II Actionable In a Phase II trial, MK2206 treatment resulted in no objective response and 1 stable disease in 7 patients with advanced breast cancer harboring PTEN loss (PMID: 31277699; NCT01277757). 31277699
FGFR2 amp stomach cancer no benefit MK2206 Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to MK2206 treatment in culture (PMID: 30045926). 30045926
BRAF V600E PIK3CA H1047R colorectal cancer predicted - sensitive MK2206 Preclinical - Cell line xenograft Actionable In a preclinical study, MK2206 treatment resulted in a modest tumor growth inhibition in a cell line xenograft model of colorectal cancer harboring BRAF V600E and PIK3CA H1047R (PMID: 22180495). 22180495
PIK3CA C420R breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R in culture (PMID: 32439931). 32439931

Filtering

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  • 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"

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  • 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
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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01802320 Phase II MK2206 Akt Inhibitor MK2206 in Treating Patients With Previously Treated Colon or Rectal Cancer That is Metastatic or Locally Advanced and Cannot Be Removed by Surgery Completed USA 0
NCT01306045 Phase II Erlotinib Lapatinib MK2206 Sunitinib Selumetinib Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies Active, not recruiting USA 0


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