Vincerx Pharma Presents Data on PTEFb / CDK9 VIP152 Inhibitor
VIP152 has increased selectivity and potency over other developing CDK9 inhibitors, consistent in DLBCL and LLC disease models
Vincerx is hosting the KOL webinar today, Saturday, December 11, 2021, 7:30 p.m. EST
PALO ALTO, Calif., December 11, 2021 (GLOBE NEWSWIRE) – Vincerx Pharma, Inc. (Nasdaq: VINC), a biopharmaceutical company aspiring to meet the unmet medical needs of cancer patients through paradigm shift therapies, today announced data on VIP152, the Company’s PTEFb / CDK9 inhibitor, in high-grade B-cell lymphoma (HGBL), formerly known as double-hit lymphoma (DHL), and chronic lymphocytic leukemia ( LLC), in two presentations at 63e The American Society of Hematology (ASH) annual meeting was held December 11-14, 2021 in Atlanta, Georgia.
“Data presented to ASH shows that VIP152 has increased selectivity and potency over other developing CDK9 inhibitors in high-grade B-cell lymphoma and chronic lymphocytic leukemia disease models.” said Ahmed Hamdy MD, CEO of Vincerx, “The consistency of the preclinical data is remarkable, with robust effects on key biomarkers of CDK9 inhibition, including the sustained downregulation of RNA polymerase II as well as sustained reduction and virtual elimination of mRNA and MYC and MCL-1 protein. These results are also reflected in primary patient samples, with VIP152 demonstrating cytotoxic activity that overcomes stromal protection in primary CLL samples, and pharmacodynamic effects on key transcriptional targets seen in the blood of HGBL patients treated with VIP152. These results suggest that the demonstrated effects of VIP152 may clinically provide new treatment options for patients with MYC and MCL-1-induced malignancies. With these expanded mechanism data in hand, we are currently recruiting two studies, a phase 1b extension study in relapsed / refractory aggressive lymphoma and advanced solid tumors, and a phase 1b dose escalation in relapsed CLL. / refractory to venetoclax and BTK inhibitors.
Highlights of the presentation:
Poster presentation, entitled “VIP152, a selective CDK9 inhibitor, induces complete regression of high-grade B-cell lymphoma (HGBL) patterns and depletion of short-lived oncogenic transcripts, MYC and MCL1, with a weekly schedulePresented by Melanie Frigault, Ph.D., Vice President Translational Medicine, Vincerx, include:
- Compared with two developing oral CDK9 inhibitors, KB-0742 and atuveciclib, at equimolar concentrations, VIP152 demonstrated more potent and sustained downregulation of phosphoserine 2 on RNA polymerase II, a key biomarker to assess the mechanism of action of CDK9 inhibitors (50% reduction over 24 to 48 hours). In addition, depletion of MYC and short half-life MCL-1 transcription levels up to 48 hours has been observed.
- VIP152 treatment conferred a change in the transcriptional program, supporting an oncogenic shock mechanism of action, and supported robust reduction and near elimination of MYC and MCL-1 proteins in MYC overexpressing lymphoma cell lines.
- Once-weekly treatment with VIP152 demonstrated antitumor efficacy as demonstrated by dose-dependent tumor regression and control of tumor outgrowth in the SU-DHL-10 xenograft model (a cell line overexpressing MYC).
- The pharmacodynamic effect demonstrated in the blood of LGBL patients treated with VIP152 suggests that the effect may be clinically manifest. Tumor-based pharmacodynamic studies are planned to confirm these results.
- VIP152 is currently being evaluated in patients with HGBL and other clinical indications expressing MYC (ClinicalTrials.gov Identifier: NCT02635672).
Oral presentation entitled “VIP152 is a new CDK9 inhibitor effective in chronic lymphocytic leukemia ” presented by Steven Sher, The Ohio State University Comprehensive Cancer Center, includes:
- VIP152 shows selective inhibition of CDK9 with improved activity compared to other CDK9 inhibitors in development, including dinaciclib, KB-0742 and atuveciclib.
- VIP152 induces apoptosis in CLL cell lines and demonstrates cytotoxic activity that overcomes stromal protection in primary CLL samples.
- VIP152 disrupts the transcriptomics of patient samples after a two hour treatment, alters cell programming, and disrupts the binding of CDK9 to canonical binding partners, thereby inhibiting its function.
- Weekly administration of VIP152 decreases peripheral disease in a mouse model of circulating tumor CLL and improves survival.
- The data supports the ongoing CLL clinical trial (ClinicalTrials.gov Identifier: NCT04978779).
Vincerx will be hosting a KOL webinar today at 7:30 p.m. Eastern Standard Time. The webinar will feature presentations from KOLs John C. Byrd, MD (University of Cincinnati) and Rosa Lapalombella, Ph.D. (The Ohio State University) who will discuss the current therapeutic landscape and unmet medical needs in the treatment of patients with of LLC and VIP152 data presented earlier today at the ASH annual meeting. Vincerx Pharma’s Vice President of Translational Medicine, Melanie Frigault, Ph.D., will also discuss the mechanism of action of VIP152 in lymphoma, poster presented to ASH
A live question-and-answer session will follow the formal presentations. To register for the webinar, please click here.
The poster is available in the presentations section of the Vincerx website.
About Vincerx Pharma, Inc.
Vincerx Pharma, Inc. (Vincerx) is a clinical-stage life sciences company focused on leveraging its extensive development and oncology expertise to advance new therapies to address unmet medical needs for treatment cancer. Vincerx has assembled a management team of biopharmaceutical experts with extensive experience building and operating organizations that develop and deliver innovative medicines to patients. Vincerx’s current pipeline is derived from an exclusive licensing agreement with Bayer and includes a clinical and follow-up small molecule drug program and a preclinical stage bioconjugation platform, which includes antibody-drug conjugates from new generation and innovative conjugates of small molecule drugs. For more information, please visit www.vincerx.com.
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