Vincerx Pharma Announces Compelling Clinical Efficacy of Enitociclib in Combination with Venetoclax and Prednisone in Lymphoma - Seite 2

About Enitociclib

Enitociclib is a highly selective CDK9 inhibitor that prevents activation of RNA polymerase II, resulting in reduction of known oncogenes MYC and MCL1 (Frigault 2023). It is currently in a dose-escalation Phase 1 trial (NTC05371054), in collaboration with the National Institutes of Health, evaluating the combination of enitociclib, venetoclax, and prednisone in DLBCL and PTCL. Two patients out of three (67%) with PTCL have had a best response of PR. A subject with angioimmunoblastic T-cell lymphoma treated in the first dose level of enitociclib had a PR with a 91% reduction in tumor burden and remains on study for follow-up. A second subject with PTCL who received the second dose level of enitociclib remains on study with a PR with an 86% reduction in pulmonary lesions and resolution of skin lesions. In addition, on the second dose cohort of enitociclib, one patient with DH-DLBCL has achieved a PR after only one cycle of treatment—highlighting the faster response rate with the combination, compared with enitociclib monotherapy. Investigators are pleased with the safety profile of this novel combination (no DLTs have been observed so far) and continue with enrollment. Early-stage clinical studies (n=95) in patients with hematologic malignancies and solid tumors provided enitociclib monotherapy proof-of-concept. Additional combination studies will be determined based on financing/partnering support.

About VIP236

VIP236, the first-in-class small molecule drug conjugate (SMDC) from our VersAptx Platform, consists of an αvβ3 integrin binder, a neutrophil elastase linker cleaved in the tumor microenvironment, and a camptothecin payload optimized for high permeability and low efflux. VIP236 was designed to deliver its payload to advanced/metastatic tumors that express αvβ3. Preclinical data show enhanced efficacy, independent of HER2 status, in patient-derived and cell line-derived gastric cancer models compared with ENHERTU, an approved ADC. VIP236 is being evaluated in a Phase 1 dose-escalation trial treating patients with advanced or metastatic solid tumors (NTC05371054). As VIP236 is a first-in-class drug, the Phase 1 trial is evaluating various dosing schedules. To date, 15 patients with advanced or metastatic disease that has relapsed or is refractory to standard of care have received VIP236; the early safety profile of once every three-week dosing is promising. This schedule also shows early signs of clinical activity. We expect to report preliminary clinical trial data in early 2024.