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PMID | |
Authors | L. Kessler et al. |
Title | KO-947, a potent and selective ERK inhibitor with slow dissociation kinetics |
Journal | European Journal of Cancer |
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Date | |
URL | http://www.ejcancer.com/article/S0959-8049(16)32974-4/abstract |
Abstract Text |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Therapy Name | Drugs | Efficacy Evidence | Clinical Trials |
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Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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KO-947 | KO947|KO 947 | ERK Inhibitor (pan) 17 | KO-947 is an inhibitor of both ERK 1 and 2, which results in inhibition of Erk signaling, thereby potentially blocking cell proliferation and inducing tumor regression (EJC Dec 2016, 69:1; S126, PMID: 30794926). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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BRAF mutant | Advanced Solid Tumor | predicted - sensitive | KO-947 | Preclinical - Pdx | Actionable | In a preclinical study, KO-947 resulted in tumor regression in patient derived xenograft (PDX) models harboring either a BRAF mutation, NRAS mutation, or KRAS mutation (EJC Dec 2016, 69:1; S126). | detail... |
NRAS mutant | Advanced Solid Tumor | predicted - sensitive | KO-947 | Preclinical - Pdx | Actionable | In a preclinical study, KO-947 resulted in tumor regression in patient derived xenograft (PDX) models harboring either a BRAF mutation, NRAS mutation, or KRAS mutation (EJC Dec 2016, 69:1; S126). | detail... |