Piperazines

TRIO Completes Enrolment for Phase 2 Giredestrant Early Breast Cancer Trial Ahead of Schedule

Retrieved on: 
Tuesday, July 6, 2021
Chemical compounds, Organic compounds, Drugs, Protein kinase inhibitors, Breakthrough therapy, Piperazines, Cyclopentanes, Lactams, Palbociclib, Breast cancer, Conjugated estrogens, Cancer research

The trial is investigating the ability to expand the safety and efficacy of giredestrant as monotherapy and in combination with palbociclib into the early breast cancer setting.

Key Points: 
  • The trial is investigating the ability to expand the safety and efficacy of giredestrant as monotherapy and in combination with palbociclib into the early breast cancer setting.
  • The trial design evaluates the efficacy, safety, and pharmacokinetics of presurgical treatment with giredestrant plus palbociclib compared with anastrozole plus palbociclib for postmenopausal women with ER+ and HER2-negative untreated early breast cancer.
  • The scale of interest from patients further underlines the urgency to bring forward new treatment options to treat early stage breast cancer.
  • TRIO advances translational cancer research by introducing innovative and novel targeted therapeutic concepts into the clinical trial setting.

Aerovate Therapeutics Announces Closing of Initial Public Offering with Exercise in Full of the Underwriters’ Option to Purchase Additional Shares

Retrieved on: 
Friday, July 2, 2021
Clinical medicine, Hypertension, Piperazines, Anatomy, Medicine, Pulmonary hypertension, Imatinib, PAH, Pulmonary artery

The aggregate gross proceeds from the offering, before deducting underwriting discounts and commissions and other estimated offering expenses payable by Aerovate, were approximately $139.8 million.

Key Points: 
  • The aggregate gross proceeds from the offering, before deducting underwriting discounts and commissions and other estimated offering expenses payable by Aerovate, were approximately $139.8 million.
  • All of the shares in the offering were sold by Aerovate.
  • Aerovate is a clinical stage biopharmaceutical company focused on developing drugs that meaningfully improve the lives of patients with rare cardiopulmonary disease.
  • Aerovate's initial focus is on advancing AV-101, its dry powder inhaled formulation of the drug imatinib for the treatment of pulmonary arterial hypertension, or PAH.

OWP Pharmaceuticals Announces Patent Issuance for the First-Ever Oral Liquid Suspension of Quetiapine for the Treatment of Schizophrenia and Bipolar Disorder

Retrieved on: 
Thursday, July 1, 2021
Psychoactive drugs, Receptor antagonists, Drugs, Atypical antipsychotics, Mood stabilizers, Piperazines, Depression, Mood disorders, Quetiapine, Antipsychotic, Bipolar I disorder, Bipolar II disorder

OWP announced today that the United States Patent and Trademark Office (USPTO) has issued a patent to OWP for the first-ever oral liquid suspension of quetiapine.

Key Points: 
  • OWP announced today that the United States Patent and Trademark Office (USPTO) has issued a patent to OWP for the first-ever oral liquid suspension of quetiapine.
  • Quetiapine is an atypical antipsychotic and the tablets, for oral use, were first approved in the U.S. in 1997.
  • In schizophrenia, quetiapine is indicated for treatment in adolescents aged 13 to 17 years and adults.
  • It is also indicated as monotherapy for the acute treatment of depressive episodes in adult patients with bipolar I and bipolar II disorder.

Resolution Bioscience (a part of Agilent) Investigated Acquired Resistance to KRAS G12C Inhibition

Retrieved on: 
Monday, June 28, 2021
Science, Biotechnology, Research, Pharmaceutical, Oncology, Health, Genetics, Clinical trials, KRAS, Piperazines, Clinical medicine, Medicine, DNA, Adagrasib, Medical specialties, Circulating free DNA, Drug resistance, Cancer

The paper was published in the New England Journal of Medicine (NEJM) on June 24 and is titled "Acquired Resistance to KRAS G12C Inhibition in Cancer."

Key Points: 
  • The paper was published in the New England Journal of Medicine (NEJM) on June 24 and is titled "Acquired Resistance to KRAS G12C Inhibition in Cancer."
  • KRAS G12C inhibitors, such as adagrasib, have shown promising efficacy in clinical trials, however, mechanisms of acquired resistance are not yet fully understood.
  • Leveraging cell-free DNA (cfDNA) analysis, this study was conducted to investigate mutations that arise that may confer resistance to patients treated with KRAS inhibitors, including adagrasib and to better understand the process of acquired resistance and to identify new strategies to combat acquired resistance.
  • The results of the study showed KRAS G12C cancers have diverse genomic and histologic mechanisms, including point mutations, copy number changes, and fusions, that appear to impart resistance to KRAS G12C inhibitors.

Research showed that InxMed FAK Inhibitor (IN10018) Overcomes Drug Resistance of KRAS G12C inhibitors and Synergizes with KRAS G12C inhibitors in Treating Cancer

Retrieved on: 
Friday, June 25, 2021
Chemical compounds, Piperazines, KRAS, Organic compounds, Antineoplastic drugs, Breakthrough therapy, Orphan drugs, Sotorasib, Targeted covalent inhibitors, Adagrasib

It can simultaneously reduce the extent of drug resistance to improve treatment outcomes of KRAS G12C inhibitors.

Key Points: 
  • It can simultaneously reduce the extent of drug resistance to improve treatment outcomes of KRAS G12C inhibitors.
  • Diverse CDX and PDX models of KRAS G12C mutant cancers were tested and synergistic benefits from the combination therapy of KRAS G12C inhibitors (AMG510 or MRTX849) and FAK inhibitor (IN10018) were consistently observed.
  • Mechanistically, it is found that aberrant FAKYAP signaling leading to the development of KRAS G12C inhibitor resistance.
  • Dr. Zaiqi Wang, InxMed's Chairman and CEO, said "This study showed that FAK inhibitor (IN10018) overcomes drug resistance of KRAS G12C inhibitors and provides a potential innovative combination therapy to improve treatment outcomes for KRAS G12C mutant cancers.

Foundation Medicine Collaborates on Research Published in The New England Journal of Medicine That Identifies Resistance to KRAS Inhibitors and Underscores Need for Novel Therapeutic Strategies

Retrieved on: 
Thursday, June 24, 2021
Biotechnology, Pharmaceutical, Health, Oncology, KRAS, Biopsy, Piperazines, FoundationOne®Liquid CDx, Foundation Medicine, FOUNDATIONONE®LIQUID CDX, FOUNDATION MEDICINE

The study found a complex landscape of acquired resistance mechanisms, with putative resistance mechanisms identified in 45% of patients.

Key Points: 
  • The study found a complex landscape of acquired resistance mechanisms, with putative resistance mechanisms identified in 45% of patients.
  • Study findings support the need for development of additional KRAS inhibitors and combination treatment strategies and reinforce the utility of liquid biopsy assays in evaluating resistance.
  • The study, Acquired Resistance to KRAS G12C Inhibition in Cancer, was published yesterday in The New England Journal of Medicine .
  • The findings suggest a diverse landscape of KRAS G12C inhibitor resistance mechanisms, which can help inform novel therapeutic strategies to effectively overcome this drug resistance in patients with cancer.

Ivy Brain Tumor Center Announces Interim Results from a Phase 0 ‘Trigger’ Trial of Targeted Combination Therapy for Glioblastoma

Retrieved on: 
Friday, June 4, 2021
Health sciences, Chemical compounds, Health, Breakthrough therapy, Piperazines, Protein kinase inhibitors, Brain tumor, Abemaciclib, Clinical trial, University of Miami Division of Surgical Neurooncology, Atypical teratoid rhabdoid tumor

In this ongoing Phase 0 study, patients receive six days of abemaciclib in combination with LY3214996 leading up to a timed brain tumor resection following the final dose.

Key Points: 
  • In this ongoing Phase 0 study, patients receive six days of abemaciclib in combination with LY3214996 leading up to a timed brain tumor resection following the final dose.
  • To date, 19 patients have enrolled in this Phase 0 clinical trial and six patients have advanced to Phase 2.
  • Additional clinical trial information can be found at NCT04391595 or the Ivy Brain Tumor Centers website .
  • Follow the Ivy Brain Tumor Center on Facebook , Instagram , Twitter and LinkedIn .

Alkermes Announces FDA Approval of LYBALVI™ for the Treatment of Schizophrenia and Bipolar I Disorder

Retrieved on: 
Tuesday, June 1, 2021
Receptor antagonists, Serotonin antagonists, Drugs, Atypical antipsychotics, Mood stabilizers, Muscarinic antagonists, Piperazines, Olanzapine, Alkermes, Schizophrenia, Olanzapine/samidorphan

"Schizophrenia and bipolar I disorder are complex, chronic diseases and there remains a persistent need for new medications with proven efficacy and safety.

Key Points: 
  • "Schizophrenia and bipolar I disorder are complex, chronic diseases and there remains a persistent need for new medications with proven efficacy and safety.
  • "LYBALVI represents an important new treatment option for adults with schizophrenia or bipolar I disorder, their clinicians and caregivers, and reflects Alkermes' commitment to developing new therapies that support patient-centered care," said Richard Pops, Chairman and Chief Executive Officer at Alkermes.
  • The most common adverse events (AEs) for both the LYBALVI and olanzapine treatment groups were weight gain, somnolence and dry mouth.
  • ENLIGHTEN-2 evaluated the weight gain profile of LYBALVI compared to olanzapine over six months in 561 patients with stable schizophrenia.

Alkermes Announces FDA Approval of LYBALVI™ for the Treatment of Schizophrenia and Bipolar I Disorder

Retrieved on: 
Tuesday, June 1, 2021
Receptor antagonists, Serotonin antagonists, Drugs, Atypical antipsychotics, Mood stabilizers, Muscarinic antagonists, Piperazines, Olanzapine, Alkermes, Schizophrenia, Olanzapine/samidorphan

"Schizophrenia and bipolar I disorder are complex, chronic diseases and there remains a persistent need for new medications with proven efficacy and safety.

Key Points: 
  • "Schizophrenia and bipolar I disorder are complex, chronic diseases and there remains a persistent need for new medications with proven efficacy and safety.
  • "LYBALVI represents an important new treatment option for adults with schizophrenia or bipolar I disorder, their clinicians and caregivers, and reflects Alkermes' commitment to developing new therapies that support patient-centered care," said Richard Pops, Chairman and Chief Executive Officer at Alkermes.
  • The most common adverse events (AEs) for both the LYBALVI and olanzapine treatment groups were weight gain, somnolence and dry mouth.
  • ENLIGHTEN-2 evaluated the weight gain profile of LYBALVI compared to olanzapine over six months in 561 patients with stable schizophrenia.

G1 Therapeutics Announces Upcoming Data at the American Society of Clinical Oncology (ASCO) Virtual 2021 Annual Meeting

Retrieved on: 
Wednesday, May 19, 2021
Chemical compounds, Organic compounds, Protein kinase inhibitors, Breakthrough therapy, Piperazines, G1 Therapeutics, Antiestrogens, Selective estrogen receptor degrader, Trilaciclib, Palbociclib, Small-cell carcinoma

b'RESEARCH TRIANGLE PARK, N.C., May 19, 2021 (GLOBE NEWSWIRE) -- G1 Therapeutics, Inc. (Nasdaq: GTHX ), a commercial-stage oncology company, today announced upcoming data presentations at the American Society of Clinical Oncology (ASCO) annual meeting, being held virtually June 4th through 8th.

Key Points: 
  • b'RESEARCH TRIANGLE PARK, N.C., May 19, 2021 (GLOBE NEWSWIRE) -- G1 Therapeutics, Inc. (Nasdaq: GTHX ), a commercial-stage oncology company, today announced upcoming data presentations at the American Society of Clinical Oncology (ASCO) annual meeting, being held virtually June 4th through 8th.
  • The presentations will describe results from the Company\xe2\x80\x99s study of its oral selective estrogen receptor degrader (SERD), rintodestrant, in combination with palbociclib for the treatment of ER+/HER2- advanced breast cancer as well as data describing the effects of COSELA\xe2\x84\xa2 (trilaciclib) on T-cell activation and clonal expansion in patients with newly diagnosed extensive-stage small cell lung cancer.
  • G1 has a deep clinical pipeline and is executing a tumor-agnostic development plan evaluating COSELA in a variety of solid tumors, including colorectal, breast, lung, and bladder cancers.
  • G1 Therapeutics is based in Research Triangle Park, N.C. For additional information, please visit www.g1therapeutics.com and follow us on Twitter @G1Therapeutics .\nG1 Therapeutics\xe2\x84\xa2 and the G1 Therapeutics logo and COSELA\xe2\x84\xa2 and the COSELA logo are trademarks of G1 Therapeutics, Inc.\n'