MYC-Targeted Agent Dosed in First Patient in Early-Phase Solid Tumor Study

The first patient has been dosed in the phase 1/2 clinical trial of an oral CDK9 inhibitor targeting MYC-amplified solid tumors known as KB-0742.

The first patient has been dosed in the phase 1/2 clinical trial of an oral CDK9 inhibitor targeting MYC-amplified solid tumors known as KB-0742, according to a press release by Kronos Bio, Inc.

KB-0742 is a highly selective, orally bioavailable inhibitor of cyclin dependent kinase 9 that is being developed to treat MYC-amplified solid tumors. According to the press release, CDK9 plays an essential role in the expression and function of MYC, which is amplified in approximately 30% of solid tumors.

MYC is one of the most sought-after targets in oncology but has eluded therapeutic treatment. Scientific research has established that MYC requires CDK9 to drive its own expression and to drive expression of its target genes. At Kronos Bio, we have observed that tumor cell lines that have extra copies of the MYC gene have heightened sensitivity to KB-0742,” said Jorge DiMartino, MD, PhD, chief medical officer and executive vice president of clinical development at Kronos Bio, Inc”, in a statement.

The open-label study aims to enroll approximately 100 patients with advanced solid tumors or non-Hodgkin’s lymphoma. The study will have a dose escalation stage and an expansion stage. The dose-escalation stage will address safety, pharmacokinetics, and the pharmacodynamic profile of KB-0742. It will also seek to establish a dose schedule.

“With KB-0742’s high selectivity for CDK9 and oral bioavailability, we have a unique opportunity in this Phase 1/2 clinical trial to investigate an optimal dose and schedule designed to provide appropriate target engagement and acceptable safety that could allow us to leverage CDK9 inhibition as an approach to treating MYC-amplified cancers,” DiMartino stated, in the press release.

Initial results from the dose escalation group is expected in the fourth quarter of 2021. Initial data from the expansion cohorts is expected in 2022.

REFERENCE:

Kronos Bio announces first patient dosed in phase 1/2 clinical trial of KB-0742, an oral CDK9 inhibitor targeting MYC-amplified cancers. Kronos Bio. February 25, 2021. Accessed February 26, 2021. https://bit.ly/3svJHwr