Highly selective oral SMARCA2 degrader, PRT7732, shows robust anti-tumor activity in vivo as monotherapy and in combination with chemotherapy, at well-tolerated doses
Potentially best-in-class CDK9 inhibitor, PRT2527, in Phase 1 development, is highly effective in preclinical hematological models as monotherapy and provides improved depth and duration of response in combination with BTK/BCL2 inhibition
Next Generation CDK4/6 Inhibitor, PRT3645, is highly effective in combination with other targeted therapies in preclinical models of breast cancer, CRC and NSCLC
WILMINGTON, Del., April 09, 2024 (GLOBE NEWSWIRE) -- Prelude Therapeutics Incorporated (Nasdaq: PRLD), a clinical-stage precision oncology company, today announced the presentation of new preclinical data at the American Association for Cancer Research (AACR) Annual Meeting for its highly selective oral SMARCA2 degrader, its potentially best-in-class CDK9 inhibitor and its next-generation oral CDK4/6 inhibitor.
“These presentations demonstrate our core competencies in medicinal chemistry and cancer biology to optimize and deliver compounds to the clinic with the potential to succeed as differentiated first- and/or best-in-class new therapies,” said Andrew Combs, Ph.D., Chief Chemistry Officer at Prelude Therapeutics.
Peggy Scherle, Ph.D., Chief Scientific Officer at Prelude, stated, “Advancement of our second highly selective SMARCA2 degrader strengthens Prelude’s leadership position in the emerging use of SMARCA2 protein degradation as a potential treatment option for underserved patients with cancer. With both a first-in-class IV SMARCA2 degrader, PRT3789, in Phase 1 clinical development and now our oral SMARCA2 degrader, PRT7732, expected to enter the clinic later this year, we believe these distinct modalities may offer new therapies for patients with SMARCA4 mutations.”
Details on the poster presentations are as follows:
Title: Preclinical Characterization of PRT7732: A Highly Potent, Selective, and Orally Bioavailable Targeted Protein Degrader of SMARCA2
Summary:
Identified potent, selective, well-tolerated and orally bioavailable SMARCA2 degrader, PRT7732
PRT7732 exhibits >3000-fold selectivity for SMARCA2 over SMARCA4, with low nanomolar potency in cell based assays
Prelude completed IND-enabling studies for PRT7732 and is on track to enter Phase 1 clinical trials in the second half of 2024
Title: PRT2527, a Novel Highly Selective Cyclin-Dependent Kinase 9 (CDK9) Inhibitor, Has Potent Antitumor Activity in Combination with BTK and BCL2 Inhibition in Various Lymphoid Malignancies
Summary:
PRT2527 is efficacious as monotherapy in preclinical models of DLBCL, CLL and MCL, and combines with both BTK and BCL2 inhibition to improve depth and duration of responses
PRT2527 is currently being evaluated in a Phase I clinical trial in patients with relapsed/refractory hematologic malignancies as monotherapy and in combination with zanubrutinib (NCT05665530)
Title: The Brain Penetrant CDK4/6 Inhibitor, PRT3645, is Highly Effective in Combination with Other Targeted Therapies in Preclinical Models of Breast Cancer, CRC and NSCLC
Summary:
Next generation CDK4/6 inhibitor, PRT3645, demonstrates preclinical synergy with SERDs, as well as MEK1/2 and CDK2 inhibition
PRT3645 has the potential to improve patient outcomes when used in combination with other targeted therapies
Prelude Therapeutics is a clinical-stage precision oncology company developing innovative drug candidates targeting critical cancer cell pathways. Prelude’s diverse pipeline is comprised of highly differentiated, potentially best-in-class proprietary small molecule compounds aimed at addressing clinically validated pathways for cancers with selectable underserved patients. Prelude’s pipeline includes: an IV administered, potent and highly selective SMARCA2 degrader, PRT3789, a preclinical oral SMARCA2 selective degrader, PRT7732, a potent and highly selective CDK9 inhibitor, PRT2527, and a next generation CDK4/6 inhibitor, PRT3645.
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