Therapy Detail

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
MK2206		MK-2206\|MK 2206	Akt Inhibitor (Pan) 22	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 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 mutant	endometrial cancer	no benefit	MK2206	Phase II	Actionable	In a Phase II trial, MK2206 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 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	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
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
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
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 E545K	urinary bladder cancer	sensitive	MK2206	Preclinical - Cell line xenograft	Actionable	In a preclinical study, MK2206 increased apoptosis and inhibited viability in bladder cancer cell lines harboring PIK3CA E545K in culture and inhibited tumor growth in cell line xenograft models (PMID: 25349966).	25349966
PIK3CA N1044K	colorectal cancer	predicted - sensitive	MK2206	Preclinical - Patient cell culture	Actionable	In a preclinical study, MK2206 inhibited cell proliferation in a patient-derived colorectal cancer organoid harboring PIK3CA N1044K, along with KRAS G12D, in culture (PMID: 32376656).	32376656
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
HRAS G13R	thyroid 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
NRAS Q61R	thyroid 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 A1066V	urinary bladder cancer	resistant	MK2206	Preclinical - Cell culture	Actionable	In a preclinical study, a bladder cancer cell line harboring PIK3CA A1066V, along with KRAS and NRAS mutations, was resistant to MK2206 in culture (PMID: 25349966).	25349966
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
PIK3CA E542K	papillary thyroid 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 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
PIK3CA E542K PIK3CA E674Q	urinary bladder cancer	sensitive	MK2206	Preclinical - Cell culture	Actionable	In a preclinical study, MK2206 increased apoptosis and inhibited viability in a bladder cancer cell line harboring PIK3CA E542K and E674Q in culture (PMID: 25349966).	25349966
PIK3CA E545G	urinary bladder cancer	sensitive	MK2206	Preclinical - Cell culture	Actionable	In a preclinical study, MK2206 increased apoptosis and inhibited viability in a bladder cancer cell line harboring PIK3CA E545G in culture (PMID: 25349966).	25349966
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	thyroid 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 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 H1047R	thyroid 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 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
PIK3CA P124L	urinary bladder cancer	resistant	MK2206	Preclinical - Cell culture	Actionable	In a preclinical study, a bladder cancer cell line harboring PIK3CA P124L was resistant to MK2206 in culture (PMID: 25349966).	25349966
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 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
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 R130*	follicular thyroid 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 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
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
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 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 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
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 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

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
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	Completed	USA	0
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

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