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DRUG:

KO-947

i
Other names: KO-947, ARS-947
Company:
Araxes Pharma, Kura Oncology
Drug class:
ERK inhibitor
almost4years
First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov)
P1, N=62, Terminated, Kura Oncology, Inc. | N=100 --> 62 | Trial completion date: Dec 2020 --> Jun 2020 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2020 --> Jun 2020; Due to a strategic business decision Kura has stopped development of KO-947. Neither safety nor efficacy reasons were the cause of study termination.
Enrollment change • Trial completion date • Trial termination • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation • HRAS mutation
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KO-947
over4years
First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov)
P1, N=100, Active, not recruiting, Kura Oncology, Inc. | Trial completion date: Aug 2020 --> Dec 2020 | Trial primary completion date: Feb 2020 --> Dec 2020
Trial completion date • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation • HRAS mutation
|
KO-947
over4years
First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov)
P1, N=100, Active, not recruiting, Kura Oncology, Inc. | Recruiting --> Active, not recruiting | N=72 --> 100 | Trial completion date: Apr 2020 --> Aug 2020 | Trial primary completion date: Oct 2019 --> Feb 2020
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog) • HRAS (Harvey rat sarcoma viral oncogene homolog)
|
KRAS mutation • BRAF mutation • NRAS mutation • HRAS mutation
|
KO-947
over4years
Targeting ERK1/2 protein-serine/threonine kinases in human cancers. (PubMed, Pharmacol Res)
The best treatments include the combination of B-Raf and MEK inhibitors (dabrafenib and trametinib, encorafenib and binimetinib, vemurafenib and cobimetanib)...Ulixertinib, MK-8353, and GDC-0994 are orally effective, potent, and specific inhibitors of ERK1/2 that are in early clinical trials for the treatment of various advanced/metastatic solid tumors...The decrease in RSK phosphorylation appears to be a result of ERK inhibition and the decrease in ERK1/2 phosphorylation is related to the inability of MEK to catalyze the phosphorylation of the ERK-MK-8353 complex; these decreases characterize the ERK dual mechanism inhibition paradigm. Additional work will be required to determine whether ERK inhibitors will be successful in the clinic and are able to forestall the development of drug resistance of the MAP kinase pathway.
Review • Journal
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BRAF (B-raf proto-oncogene) • MAPK1 (Mitogen-activated protein kinase 1)
|
Mekinist (trametinib) • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • Mektovi (binimetinib) • Braftovi (encorafenib) • ulixertinib (BVD-523) • SCH772984 • KO-947 • temuterkib (LY3214996) • CC-90003 • MK-8353 • ravoxertinib (RG7842)