KO-947 News - LARVOL Sigma

|||||||||| Review, Journal: Advances in ERK1/2 inhibition: a medicinal chemistry perspective on structure and regulation. (Pubmed Central) - Sep 10, 2025
This review also highlights recent advances in the design and synthesis of ERK inhibitors, emphasising their structural uniqueness and potential to inhibit mutant forms of ERK1/2. Finally, we discuss future directions for the development of ERK1/2 inhibitors as FDA-approved cancer therapeutics.

|||||||||| KO-947 / Kura Oncology, Araxes Pharma
P1 data, Journal: A phase I, first-in-human trial of KO-947, an ERK1/2 inhibitor, in patients with advanced solid tumors. (Pubmed Central) - Mar 24, 2025
Finally, we discuss future directions for the development of ERK1/2 inhibitors as FDA-approved cancer therapeutics. Intravenous KO-947 had a generally tolerable safety profile with minimal gastrointestinal toxicity compared with oral administration of other ERK inhibitors.

|||||||||| KO-947 / Kura Oncology
Clinical, Journal: From Lab Formulation Development to CTM Manufacturing of KO-947 Injectable Drug Products: a Case Study and Lessons Learned. (Pubmed Central) - Jun 16, 2021
An unexpected stability issue was encountered, and the root cause was attributed to the heterogeneous liquid freezing process of the formulated solution at -20°C, which had not been captured in the lab setting. A lyophilized product was then designed to overcome the issue and supplied to the phase I clinical trial.

||||||||||  KO-947 / Kura Oncology, Araxes Pharma
Enrollment change, Trial completion date, Trial termination, Trial primary completion date, First-in-human:  First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov) -  Jan 26, 2021
P1, N=62, Terminated,  Sponsor: 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.

||||||||||  KO-947 / Kura Oncology, Araxes Pharma
Trial completion date, Trial primary completion date, First-in-human:  First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov) -  Jun 23, 2020
P1, N=100, Active, not recruiting,  Sponsor: Kura Oncology, Inc.
Neither safety nor efficacy reasons were the cause of study termination. Trial completion date: Aug 2020 --> Dec 2020 | Trial primary completion date: Feb 2020 --> Dec 2020

||||||||||  KO-947 / Kura Oncology, Araxes Pharma
Enrollment closed, Enrollment change, Trial completion date, Trial primary completion date, First-in-human:  First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov) -  Mar 2, 2020
P1, N=100, Active, not recruiting,  Sponsor: Kura Oncology, Inc.
Trial completion date: Aug 2020 --> Dec 2020 | Trial primary completion date: Feb 2020 --> Dec 2020 Recruiting --> Active, not recruiting | N=72 --> 100 | Trial completion date: Apr 2020 --> Aug 2020 | Trial primary completion date: Oct 2019 --> Feb 2020

|||||||||| Review, Journal: Targeting ERK1/2 protein-serine/threonine kinases in human cancers. (Pubmed Central) - Feb 16, 2020
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.

||||||||||  KO-947 / Kura Oncology, Araxes Pharma
Enrollment open, First-in-human:  First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov) -  Apr 14, 2017
P1, N=72, Recruiting,  Sponsor: Kura Oncology, Inc.
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. Not yet recruiting --> Recruiting

||||||||||  KO-947 / Kura Oncology, Araxes Pharma
New P1 trial, First-in-human:  First-in-Human Study of KO-947 in Non-Hematological Malignancies (clinicaltrials.gov) -  Feb 13, 2017
P1, N=72, Not yet recruiting,  Sponsor: Kura Oncology, Inc.



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