Selective estrogen receptor degrader

Prelude Highlights Continued Strength of Discovery Engine at 2024 AACR Annual Meeting

Retrieved on: 
Tuesday, April 9, 2024
Breast cancer, SMARCA4, MCL, Generation, Prelude, CDK2, CLL, NSCLC, Patient, SMARCA2, Selective estrogen receptor degrader, BCL2, Cancer, AACR, CRC, BTK, CDK9, DLBCL, Pharmaceutical industry

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.

Key Points: 
  • Highly selective oral SMARCA2 degrader, PRT7732, shows robust anti-tumor activity in vivo as monotherapy and in combination with chemotherapy, at well-tolerated doses
    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:
    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
    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
    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
    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
    Next generation CDK4/6 inhibitor, PRT3645, demonstrates preclinical synergy with SERDs, as well as MEK1/2 and CDK2 inhibition

Olema Oncology Announces Publication of Data Highlighting Palazestrant’s Ability to Inhibit Wild-Type and Mutant ER+ Breast Cancer Both as Monotherapy and in Combination with CDK4/6 Inhibitors

Retrieved on: 
Wednesday, March 6, 2024
Paper, Combination therapy, Breast cancer, SAN, Woman, FDA, Animal, Proteolysis targeting chimera, Behavior, Therapy, Selective estrogen receptor degrader, Enzyme inhibitor, CNS, Pharmacokinetics, Survival, MOA, Research, Mutant, Pharmaceutical industry

The paper, titled “Palazestrant (OP-1250), a Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination”, describes the scientific background underlying the design, discovery and optimization of palazestrant.

Key Points: 
  • The paper, titled “Palazestrant (OP-1250), a Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination”, describes the scientific background underlying the design, discovery and optimization of palazestrant.
  • “What’s even more exciting is to see how faithfully the pre-clinical research predicted the behavior of palazestrant now that it is in late-stage clinical development.
  • In mouse xenograft models, palazestrant demonstrated excellent pharmacokinetics, was well tolerated, showed synergy with CDK4/6 inhibitors, and was highly effective at reducing tumor growth in both wild-type and ESR1-mutant ER+ breast cancer.
  • In addition, in an ESR1-mutant intercranial xenograft model, palazestrant inhibited tumor growth and improved survival of animals with CNS metastases, even after stopping drug treatment.

OnKure Announces IND Clearance by U.S. FDA Enabling Phase 1 Initiation for its Mutant Selective PI3Kα inhibitor, OKI-219

Retrieved on: 
Thursday, January 4, 2024
Food, Mutation, IND, Breast cancer, HER2, Fulvestrant, Breast, FDA, Selective estrogen receptor degrader, Tucatinib, Hyperglycemia, Clinical trial, Investigational New Drug, Cancer, Patient

H1047R is the most common mutation in PI3Kα, being found in 15% of breast cancer and 4% of cancers overall.

Key Points: 
  • H1047R is the most common mutation in PI3Kα, being found in 15% of breast cancer and 4% of cancers overall.
  • There is a significant need for improved therapies targeting PI3Kα with safer and more effective drugs.
  • Similarly, the combination of OKI-219 + tucatinib drives strong regressions in models of HER2+/ PI3Kα H1047R breast cancer that are resistant to HER2- inhibitors.
  • Subsequent evaluation of OKI-219 in combination with the SERD fulvestrant in ER+/ PI3Kα H1047R advanced breast cancer, and with the HER2-monoclonal antibody trastuzumab in HER2+/ PI3Kα H1047R advanced breast cancers will follow.

EvolveImmune Therapeutics Presents New Preclinical and Translational Data on Novel CD2 Costimulatory T Cell Engager Platform at 38th Annual Meeting of the Society for Immunotherapy of Cancer (SITC)

Retrieved on: 
Monday, November 6, 2023
Neoplasm, SERM, CD3, EVOLVE, Breast, Therapy, ULBP2, SERD, Salk Institute for Biological Studies, Immunology, Research, Selective estrogen receptor degrader, SITC, B7-H4, Immunotherapy, Estrogen receptor, Cancer, Triple-negative breast cancer, Breast cancer, TNBC, Society, Patient, CD2, Vaccine, Pharmaceutical industry

In addition, presented data highlighted the robust anti-tumor efficacy exhibited by lead molecules for the EV-104 and EV-106 programs in patient-derived solid tumor models.

Key Points: 
  • In addition, presented data highlighted the robust anti-tumor efficacy exhibited by lead molecules for the EV-104 and EV-106 programs in patient-derived solid tumor models.
  • The EVOLVE platform uniquely unleashes potent, selective and integrated T cell costimulation, which amplifies and sustains the tumor killing capacity of these T cells.
  • The platform also takes advantage the company’s understanding of specific tumor cell characteristics to guide tumor antigen prioritization and program differentiation.
  • In a poster presentation at SITC, EvolveImmune spotlighted advances to the company’s first-in-class EV-104 program, a novel multi-functional T cell engager with integrated CD2 costimulation which conditionally targets ULBP2.

Pinetree Therapeutics Announces Two Appointments to Strengthen its Scientific Leadership

Retrieved on: 
Wednesday, May 31, 2023
Therapy, Regeneron Pharmaceuticals, Seagen, Biotechnology, MedImmune, Cancer, United States Air Force Scientific Advisory Board, Janssen, TPD, Research, Bristol Myers Squibb, Doctor of Philosophy, Rutgers University, Pinetree, Selective estrogen receptor degrader, DRS, Novartis, Patient, Molecular Partners, Engineering, Boehringer Ingelheim, Immunotoxin, BMS, IND, Disease, Pharmaceutical industry, Vaccine, Bayer, Merck

CAMBRIDGE, Mass., May 31, 2023 /PRNewswire/ -- Pinetree Therapeutics, Inc. ("Pinetree" or the "Company"), an emerging and award winning biotechnology company pioneering next generation targeted protein degraders (TPD) to overcome the shortcomings of existing therapies, today announced the addition of Pamela A. Trail, PhD, to its Scientific Advisory Board as well as the appointment of John Majercak, PhD, as Chief Technology Officer.

Key Points: 
  • Trail, PhD, to its Scientific Advisory Board as well as the appointment of John Majercak, PhD, as Chief Technology Officer.
  • "I am pleased to join the Scientific Advisory Board at Pinetree Therapeutics at this exciting time", said Dr.
  • "The novel platforms at Pinetree Therapeutics provide unique opportunities to develop therapeutics for treatment of diseases with high unmet medical need."
  • Dr. Majercak added, "I am thrilled to join Pinetree Therapeutics to help bring new treatment options to cancer patients.

Mays Cancer Center led studies of innovative breast cancer drug that recently gained FDA approval

Retrieved on: 
Wednesday, February 1, 2023
UT Health San Antonio Cancer Center, Woman, NCI, Doctor of Philosophy, Standard of care, Pharmacotherapy, National Cancer Institute, Medicine, HER2, University of Texas System, Patient, Biochemistry, Clinical trial, NCI-designated Cancer Center, Workforce, University, Food, Research, Regulation of food and dietary supplements by the U.S. Food and Drug Administration, University of Texas Health Science Center at San Antonio, FDA, Growth, SAN, MD Anderson Cancer Center, ESR1, Neoplasm, Selective estrogen receptor degrader, Cancer, MD, Pharmaceutical industry, Medical imaging, Dietary supplement

SAN ANTONIO, Feb. 1, 2023  /PRNewswire-PRWeb/ -- The Mays Cancer Center, home to UT Health San Antonio MD Anderson Cancer Center, was the lead site for a study evaluating Phase I and Phase III clinical trials for elacestrant, a treatment for postmenopausal women and adult men with ER+/HER2- advanced or metastatic breast cancer. The U.S. Food and Drug Administration on Jan. 27 announced it approved the novel drug therapy.

Key Points: 
  • The Mays Cancer Center is one of only four National Cancer Institute (NCI)-designated Cancer Centers in Texas.
  • "The FDA approval of elacestrant for the treatment of metastatic breast cancer is a strong testament to the commitment of the Mays Cancer Center toward the alleviation of cancer burden through innovative research and clinical trials," Patrick Sung, DPhil , interim executive director of Mays Cancer Center and professor of biochemistry and structural biology.
  • The Mays Cancer Center, home to UT Health San Antonio MD Anderson Cancer Center , is one of only four National Cancer Institute-designated Cancer Centers in Texas.
  • The Mays Cancer Center provides leading-edge cancer care, propels innovative cancer research and educates the next generation of leaders to end cancer in South Texas.

Systems Oncology to Present Positive Preclinical Data for SERA2 at J.P. Morgan 41st Annual Healthcare Conference

Retrieved on: 
Tuesday, December 6, 2022
Oncology, Health, Health Technology, Research, Science, Pharmaceutical, Biotechnology, ER, Chemistry, Baylor University Medical Center, UPR, Champaign County, Illinois, Oncology, J. P. Morgan, Intellectual property, IP, Patient, SERA, Research, Biology, Breast cancer, SO, Aromatase, Unfolded protein response, Selective estrogen receptor degrader, McKesson Corporation, Cell death, University, Selective estrogen receptor modulator, Medical imaging, Pharmaceutical industry

Systems Oncology today announced they will be presenting positive preclinical data on the companys next generation estrogen receptor positive drug candidate, SERA2 (Selective Estrogen Receptor Activator).

Key Points: 
  • Systems Oncology today announced they will be presenting positive preclinical data on the companys next generation estrogen receptor positive drug candidate, SERA2 (Selective Estrogen Receptor Activator).
  • In the preclinical data presented at J.P. Morgan, treatment with SERA2 in animal models of human breast cancer results in multiple, complete, durable tumor regressions.
  • These data support the rationale for SERA2 as a novel therapeutic for the treatment of breast cancer and potentially other estrogen receptor positive cancers.
  • Systems Oncology will be having partnering meetings during the J.P. Morgan conference from January 9 to January 11, 2023.

ReCode Therapeutics Appoints Trisha Millican to Board of Directors

Retrieved on: 
Thursday, December 1, 2022
Health, Genetics, General Health, Research, Science, Pharmaceutical, Biotechnology, Selective estrogen receptor degrader, Financial management, Cancer, University, RNA, Cell, Therapy, MBA, Recode, Disease, RNA transfection, SORT, Sale, Cystic fibrosis, LNP, Johnson & Johnson, Liver, Pharmaceutical industry, Management, Vaccine, Genentech

ReCode Therapeutics, a genetic medicines company using superior delivery to power the next wave of mRNA and gene correction therapeutics, announced today the appointment of Patricia Trisha Millican to the companys Board of Directors.

Key Points: 
  • ReCode Therapeutics, a genetic medicines company using superior delivery to power the next wave of mRNA and gene correction therapeutics, announced today the appointment of Patricia Trisha Millican to the companys Board of Directors.
  • On behalf of ReCodes leadership team and Board, I am delighted to welcome Trisha Millican to our Board of Directors, said Shehnaaz Suliman, M.D., MBA, M.Phil., chief executive officer and a board member of ReCode Therapeutics.
  • Currently, Ms. Millican is a strategic advisor to various life science companies and serves on the board of directors of Life Science Cares, San Diego.
  • ReCode Therapeutics is a genetic medicines company using superior delivery to power the next wave of messenger RNA (mRNA) and gene correction therapeutics.

Selective Estrogen Receptor Degraders Drug Pipeline Research Report 2022 - ResearchAndMarkets.com

Retrieved on: 
Monday, August 1, 2022
Women, Consumer, Health, Pharmaceutical, Oncology, Genentech, III, Estrogen, Route, Discovery, SERD, News, Clinical trial, Administration, Patient, Breast cancer, Therapy, Route of administration, II, Selective estrogen receptor degrader, Birth control, Pharmaceutical industry

The "Selective estrogen receptor degraders - Pipeline Insight, 2022" clinical trials has been added to ResearchAndMarkets.com's offering.

Key Points: 
  • The "Selective estrogen receptor degraders - Pipeline Insight, 2022" clinical trials has been added to ResearchAndMarkets.com's offering.
  • This "Selective Estrogen Receptor Degraders - Pipeline Insight, 2022" report provides comprehensive insights about 14+ companies and 14+ pipeline drugs in the Selective Estrogen Receptor Degraders pipeline landscape.
  • This segment of the report provides insights about the different Selective Estrogen Receptor Degraders drugs segregated based on following parameters that define the scope of the report.
  • The Selective Estrogen Receptor Degraders pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration.

Zentalis Pharmaceuticals Announces Positive Initial Clinical Data on ZN-c3, its Wee1 Inhibitor, in Patients with Advanced Ovarian Cancer at AACR

Retrieved on: 
Friday, April 8, 2022
Company, Private Securities Litigation Reform Act, Vomiting, Drug development, Cancer, Abstract, Population, Therapy, DDI, Interim, PARP, University of Oklahoma College of Medicine, DNA, Investor, AML, Cell death, DNA repair, Selective estrogen receptor degrader, SEC, EDT, Standard of care, Associate, Failure, Nausea, NSCLC, Osteosarcoma, EGFR, Ovarian cancer, MD, Neutropenia, Thrombocytopenia, Anemia, Safety, Biology, U.S. Securities and Exchange Commission, Western Airlines Flight 2605, CDK, Jim, COVID-19, SERD, Large-cell lung carcinoma, Gynecologic Oncology (journal), FDA, Breast cancer, Annual report, University, Patient, Toxicity, Pharmaceutical industry, Aluminium, USC, Wee1

Wee1 inhibition remains a promising therapeutic approach to treating an array of solid tumors, including advanced ovarian cancer, and these results further support the class potential in changing the treatment paradigm.

Key Points: 
  • Wee1 inhibition remains a promising therapeutic approach to treating an array of solid tumors, including advanced ovarian cancer, and these results further support the class potential in changing the treatment paradigm.
  • Interim data from the Phase 1 monotherapy USC expansion cohort receiving ZN-c3 300mg QD were also released today.
  • ZN-c3 is potentially a best-in-class Wee1 inhibitor and is in an ongoing potentially registrational Phase 2 trial for USC patients (NCT04814108).
  • Zentalis plans to initiate a combination study of ZN-c5 + ZN-c3 in ER+/HER2- CDK 4/6i-resistant breast cancer patients in 2022.