SAN DIEGO, CA, USA I January 6, 2016 I eFFECTOR Therapeutics, Inc., a biopharmaceutical company developing selective translation regulators for the treatment of cancer, today announced that dosing has begun in a Phase 1/2 dose-escalation and cohort-expansion study of eFT508 in patients with advanced solid tumors. eFT508 is the company’s potent, highly selective oral inhibitor of MNK1 and MNK2.

“Initiation of this first clinical trial of eFT508 marks an important milestone for the program, our scientific founders and the company,” said Steve Worland, Ph.D., president and CEO of eFFECTOR. “We look forward to demonstrating target engagement, identifying a recommended Phase 2 dose and initiating expansion cohorts in specific solid tumor types during 2016. We also expect to open a second clinical trial of eFT508 in patients with lymphoma in the coming months.”

The Phase 1/2 trial is evaluating the safety, pharmacokinetics, pharmacodynamics, and antitumor activity of daily oral eFT508 in patients with advanced solid tumors. The primary endpoint for the dose-escalation portion of the study is the maximum tolerated dose (MTD) and/or recommended dose (RD). The primary endpoint for the cohort-expansion portion of the study is overall response rate (ORR) in patients with specific tumor types. Pharmacodynamic markers to be measured include phosphorylation of eIF4E, a key component of the translation initiation complex, and levels of translationally regulated tumor-driving proteins that were previously identified using eFFECTOR’s platform technology.

Additional information about the clinical trial can be found on the ClinicalTrials.gov website at the following link: https://clinicaltrials.gov/ct2/show/NCT02605083.

About eFT508

eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor. MNK1 and MNK2 integrate signals from several oncogenic and immune signaling pathways by phosphorylating eIF4E and other key messenger RNA (mRNA) binding proteins that regulate the stability and translation of select mRNAs important for tumor growth and survival. eFT508 has demonstrated substantial activity in multiple preclinical human tumor models as a monotherapy and in combination with novel targeted agents as well as drugs that are components of standard of care regimens. Data regarding the activity of eFT508 in hematologic tumor models was presented recently at the 57th Annual Meeting of the American Society of Hematology. The abstract can be found at the following link: Blood 2015; 126(23):1554 and the poster at the following link: “eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL)”.

About eFFECTOR Therapeutics

eFFECTOR Therapeutics is pioneering the discovery and development of selective translation regulators as a new class of small molecule therapeutics for cancer. The company’s investigational compounds are designed to restore translational control to halt underlying disease mechanisms while preserving healthy physiological processes. eFFECTOR’s lead drug candidate, eFT508, is a highly selective MNK1 and MNK2 inhibitor. MNK1 and 2 are kinases that act as signal integrators at the convergence of multiple oncogenic and immune signaling pathways to regulate production of disease-driving proteins. The company has additional translation regulation programs currently in discovery. eFFECTOR has raised $95M in financing from top-tier private and corporate venture funds. For more information visit www.effector.com.

SOURCE: eFFECTOR Therapeutics