MTORC1


Associated tags: Ageing, Fibrosis, Inflammation

Revolution Medicines Announces Publication Describing Design and Synthesis of RMC-5552, a First-in-Class, Bi-Steric mTORC1-Selective Inhibitor

Retrieved on: 
Monday, December 19, 2022

REDWOOD CITY, Calif., Dec. 19, 2022 (GLOBE NEWSWIRE) -- Revolution Medicines, Inc. (Nasdaq: RVMD), a clinical-stage oncology company developing targeted therapies for RAS-addicted cancers, today announced publication of a manuscript in the Journal of Medicinal Chemistry that details the discovery efforts leading to RMC-5552, the company’s first-in-class, bi-steric mTORC1-selective inhibitor. The manuscript describes the unprecedented compound profile that includes 40-fold selectivity for mTORC1 over mTORC2 and greater than 53-fold selectivity over other lipid kinases. The paper also shows that selective mTORC1 inhibition using the company’s related preclinical tool compound (RMC-6272) in combination with a covalent KRASG12C inhibitor induced tumor regressions in a preclinical model of KRASG12C mutant non-small cell lung cancer (NSCLC) that exhibits resistance to KRASG12C inhibitor monotherapy.

Key Points: 
  • The manuscript describes the unprecedented compound profile that includes 40-fold selectivity for mTORC1 over mTORC2 and greater than 53-fold selectivity over other lipid kinases.
  • RMC-5552 is designed to suppress phosphorylation and inactivation of 4EBP1, a key translational regulator of oncogene expression, in cancers with hyperactive mTORC1 signaling.
  • Revolution Medicines is currently evaluating RMC-5552 as monotherapy in a Phase 1/1b clinical trial in patients with refractory solid tumors ( NCT04774952 ), and initial antitumor activity has been reported.
  • “The Journal of Medicinal Chemistry manuscript details the sophisticated structure-based chemical design and synthesis employed by our drug discovery team that produced RMC-5552,” said Steve Kelsey, M.D., president, research and development at Revolution Medicines.

Navitor Pharmaceuticals Announces Janssen Has Acquired Anakuria Therapeutics, Inc.

Retrieved on: 
Wednesday, February 2, 2022

Today, privately held Navitor Pharmaceuticals, LLC (Navitor), announced that Janssen Pharmaceuticals, Inc. (Janssen), one of the Janssen Pharmaceutical Companies of Johnson & Johnson has acquired Anakuria Therapeutics, Inc., (Anakuria), a company recently formed by Navitor to advance its novel class of selective rapamycin analog mTORC1 inhibitors.

Key Points: 
  • Today, privately held Navitor Pharmaceuticals, LLC (Navitor), announced that Janssen Pharmaceuticals, Inc. (Janssen), one of the Janssen Pharmaceutical Companies of Johnson & Johnson has acquired Anakuria Therapeutics, Inc., (Anakuria), a company recently formed by Navitor to advance its novel class of selective rapamycin analog mTORC1 inhibitors.
  • Under the terms of the agreement, Janssen has acquired all outstanding shares of Anakuria, which is now a wholly owned subsidiary of Janssen.
  • Tom Hughes, president and chief executive officer of Navitor Pharmaceuticals LLC commented, "We are thrilled that the potential value and substantially differentiated profile of Anakurias mTORC1 inhibitor program can be explored with Janssen.
  • Navitor Pharmaceuticals, LLC, the parent company for Navitor Pharmaceuticals, Inc., is the leader in the development of mTORC1-targeted therapeutics designed to help patients live longer and healthier lives.

Navitor’s Three Phase 1 Studies for NV-5138 Show Antidepressant Effects and Biomarker Impact, Supporting Further Development of Direct Activator of mTORC1 in Depression

Retrieved on: 
Thursday, September 12, 2019

The Phase 1 NV-5138 program consisted of three randomized, placebo-controlled, double-blinded studies (001, 002, 003) measuring the safety, tolerability and pharmacokinetics of orally administered NV-5138.

Key Points: 
  • The Phase 1 NV-5138 program consisted of three randomized, placebo-controlled, double-blinded studies (001, 002, 003) measuring the safety, tolerability and pharmacokinetics of orally administered NV-5138.
  • For people battling depression, theres a real need for fast acting relief of symptoms so that they can begin the journey of getting well again.
  • We are particularly impressed with the consistent impact of a single dose of NV-5138 in all three studies.
  • NV-5138 binds to and modulates sestrin, which senses amino acid availability in the brain, a potent natural activator of mTORC1.

Navitor Expands Leadership Team with Appointment of James Randall Owen, M.D. as Chief Medical Officer

Retrieved on: 
Monday, July 15, 2019

as the Companys first Chief Medical Officer.

Key Points: 
  • as the Companys first Chief Medical Officer.
  • At Navitor, Randy will be responsible for the clinical and regulatory development of Navitors pipeline of product candidates and will report to Thomas E. Hughes, Ph.D., the Companys Chief Executive Officer.
  • We are thrilled to welcome Randy to the Navitor team.
  • Navitor Pharmaceuticals, Inc. is the leader in the development of mTORC1-targeted therapeutics designed to help patients live longer and healthier lives.