VIP236 is a first-in-class anticancer agent, optimized using Vincerx’s proprietary modular bioconjugation platform to target aggressive tumors
VIP236 demonstrates promising tumor regression in in vivo cancer models and is currently in IND-enabling studies
PALO ALTO, Calif., Feb. 03, 2022 (GLOBE NEWSWIRE) -- Vincerx Pharma, Inc. (Nasdaq: VINC), a biopharmaceutical company aspiring to address the unmet medical needs of patients with cancer through paradigm-shifting therapeutics, today announced the publication of a peer-reviewed article titled, “A Small Molecule–Drug Conjugate (SMDC) Consisting of a Modified Camptothecin Payload Linked to an αVß3 Binder for the Treatment of Multiple Cancer Types” in the special issue “The Role of Tumor Microenvironment in Solid Tumors: The New Frontier of Cancer Research” of the journal Cancers. The preclinical data in the paper highlight the potential of VIP236, a small molecule-drug conjugate (SMDC), to directly target cancer cells, while reducing the harmful effects of chemotherapy to normal tissue.
“These preclinical data provide compelling proof-of-concept that our novel SMDC, VIP236, can direct a potent cancer chemotherapy drug to tumors while sparing healthy tissues,” said Ahmed Hamdy M.D., Chief Executive Officer of Vincerx. “We have a diverse, modular platform of linkers and payloads that can be conjugated with typical antibodies or small molecules, creating the potential for novel drugs with greater efficacy and lower toxicities than current antibody-drug conjugates; VIP236 is an example of the strength of this platform.”
VIP236 tumor homing is guided by an αVß3 integrin ligand, which targets mechanisms that drive aggressive and invasive cancers. The published results provide preclinical validation of this targeting strategy and demonstrate how this approach can deliver 40 times more drug to the cancer than the surrounding tissues or normal organs. VIP236 is further activated by another component prevalent in the tumor microenvironment of invasive cancers, neutrophil elastase, which cleaves the linker, releasing a potent payload directly in the tumor microenvironment. The payload is a differentiated camptothecin (CPT) optimized to be more cell permeable and to overcome drug resistance observed with traditional CPTs.
Dr. Hamdy continued, “Our promising in vivo mouse data across various tumor types highlight the potential of our rationally designed SMDC to transform the treatment paradigm for advanced solid tumors. We look forward to advancing VIP236 into the clinic in the second half of 2022.”
Key Article Highlights Include:
- The αVß3 integrin targeting strategy in VIP236 increases tumor homing by 42-fold as measured by a fluorescent dye conjugated to the integrin targeting moiety and demonstrated in a human renal cell carcinoma (786-O) xenografted mouse model.
- The cytotoxic payload of VIP236, VIP126, is an optimized CPT which shows improvement in permeability, efflux ratio and cytotoxicity in drug transporter overexpressing cancer cells compared with SN38, a clinically validated CPT. Unlike SN38, VIP126 is a very poor substrate for P-gp- or BCRP-mediated efflux transport, which translated into greater efficacy.
- VIP236 in vitro cytotoxic activity against tumor cell lines is neutrophil elastase (NE) dependent.
- Neutrophil elastase, prevalent in the tumor microenvironment, cleaves the linker, to release the anticancer payload within the tumor.
- VIP236 results in a ten-fold higher tumor-to-plasma ratio of the payload, VIP126, when compared to direct administration of VIP126 in vivo, highlighting a potential therapeutic advantage of the conjugate delivery system.
- Compared with commonly used chemotherapeutics, VIP236 shows very effective tumor targeting, better tumor regression, and better tolerability in mouse models of triple negative breast cancer, small cell lung cancer and colorectal cancer.
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 intended to address unmet medical needs for the treatment of cancer. Vincerx has assembled a management team of biopharmaceutical experts with extensive experience in building and operating organizations that develop and deliver innovative medicines to patients. Vincerx’s current pipeline is derived from an exclusive license agreement with Bayer and includes a clinical-stage and follow-on small molecule drug program and a preclinical stage modular bioconjugation platform, which includes next-generation antibody-drug conjugates and innovative small molecule drug conjugates. For more information, please visit www.vincerx.com.
Cautionary Statement
This press release contains forward-looking statements within the meaning of Section 27A of the Securities Act of 1933, as amended (the “Securities Act”), and Section 21E of the Securities Exchange Act of 1934, as amended, that are intended to be covered by the “safe harbor” created by those sections. Forward-looking statements, which are based on certain assumptions and describe future plans, strategies, expectations and events, can generally be identified by the use of forward-looking terms such as “believe,” “expect,” “may,” “will,” “should,” “would,” “could,” “suggest,” “seek,” “intend,” “plan,” “goal,” “potential,” “project,” “estimate,” “anticipate” or other comparable terms. All statements other than statements of historical facts included in this press release are forward-looking statements. Forward-looking statements include, but are not limited to: Vincerx’s business model, pipeline, strategy, timeline, product candidates and preclinical and clinical development and results. Forward-looking statements are neither historical facts nor assurances of future performance or events. Instead, they are based only on current beliefs, expectations and assumptions regarding future business developments, future plans and strategies, projections, anticipated events and trends, the economy and other future conditions. Forward-looking statements are subject to inherent uncertainties, risks and changes in circumstances that are difficult to predict and many of which are outside of our control.
Actual results, conditions and events may differ materially from those indicated in the forward-looking statements. Therefore, you should not rely on any of these forward-looking statements. Important factors that could cause actual results, conditions and events to differ materially from those indicated in the forward-looking statements include, but are not limited to: general economic, financial, legal, political and business conditions and changes in domestic and foreign markets; the potential effects of the COVID-19 pandemic; risks associated with preclinical or clinical development and trials, including those conducted prior to Vincerx’s in-licensing; failure to realize the benefits of Vincerx’s license agreement with Bayer; risks related to the rollout of Vincerx’s business and the timing of expected business milestones; changes in the assumptions underlying Vincerx’s expectations regarding its future business or business model; Vincerx’s ability to develop and commercialize product candidates; the availability and uses of capital; the effects of competition on Vincerx’s future business; and the risks and uncertainties set forth in Forms 10-K, 10-Q and 8-K filed with or furnished to the SEC from time to time by Vincerx. Forward-looking statements speak only as of the date hereof, and Vincerx disclaims any obligation to update any forward-looking statements.
Contacts
Bruce Mackle
LifeSci Advisors, LLC
646-889-1200
bmackle@lifesciadvisors.com
