On October 29, 2019 Tolero Pharmaceuticals, Inc., a clinical-stage company focused on developing novel therapeutics for hematological and oncological diseases, reported the presentation of preclinical data of TP-1287, an investigational oral cyclin-dependent kinase 9 (CDK9) inhibitor, in castration-sensitive and resistant prostate cancer models and TP-1454, an investigational small-molecule pyruvate kinase M2 isoform (PKM2) activator, in colorectal cancer models (Press release, Tolero Pharmaceuticals, OCT 29, 2019, View Source;in-colorectal-cancer-models-300947320.html [SID1234550000]). These data were shared at the 2019 AACR (Free AACR Whitepaper)-NCI-EORTC AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper), being held October 26-30, 2019, in Boston, Massachusetts.
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"We are pleased to present data on our early-stage investigational agents, TP-1287 and TP-1454. These results are a testament to our commitment to develop novel therapeutics and expand the combined oncology portfolio of Tolero and its parent company, Sumitomo Dainippon Pharma," said David J. Bearss, Ph.D., Chief Executive Officer of Tolero Pharmaceuticals, Inc. "Furthermore, these data improve our understanding of these assets and provide insight into the potential role CDK9 inhibition and PKM2 activation may play in the treatment of prostate and colorectal cancer."
Data from a preclinical prostate cancer model, showed TP-1287 as monotherapy and in combination with venetoclax or docetaxel enhanced tumor growth inhibition. Additionally, TP-1287 combined with docetaxel alone showed tumor growth inhibition.
In a separate preclinical colorectal cancer model, TP-1454 in combination with anti-PD1 and anti-CTLA4 therapies showed tumor regression, tumor growth inhibition and an acceptable safety profile.
Below are the details for the Tolero presentations:
Abstract Title
Details
Presenter
PKM2 Activation Modulates
Metabolism and Enhances
Immune Response in Solid
Tumor Models
Abstract #B080
October 28, 2019
12:30 – 04:00 p.m. ET
Poster Presentation
Satya Pathi, Ph.D., Study
Director in Pre-clinical
Oncology, Crown Bioscience,
Inc
Targeting CDK9 and Mcl-1 in
Castration-sensitive and
Resistant Prostate Cancer
Models
Abstract #C081
October 29, 2019
12:30 – 04:00 p.m. ET
Poster Presentation
Tetyana V. Forostyan,
Graduate Research
Assistant, Oncological
Sciences, University of Utah
About TP-1287
TP-1287 is an investigational oral cyclin-dependent kinase 9 (CDK9) inhibitor under evaluation in a Phase 1 study in patients with advanced solid tumors (NCT03604783). TP-1287 has shown favorable oral bioavailability in preclinical models.
About TP-1454
TP-1454 is an investigational oral pyruvate kinase M2 isoform (PKM2) activator, under preclinical evaluation in cell-based and animal models of solid tumors.