PF-07258669 / Pfizer 
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  • ||||||||||  PF-07258669 / Pfizer
    Journal:  Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines. (Pubmed Central) -  Oct 4, 2023   
    Altogether, this provides a highly modular access to four isomeric THN cores from a common set of unprotected primary amine starting materials, using the same bond disconnections. The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core of Pfizer's MC4R antagonist PF-07258669.
  • ||||||||||  PF-07258669 / Pfizer
    Trial completion, Enrollment change:  A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) -  Aug 22, 2023   
    P1,  N=40, Completed, 
    The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core of Pfizer's MC4R antagonist PF-07258669. Recruiting --> Completed | N=150 --> 40
  • ||||||||||  PF-07258669 / Pfizer
    Trial completion date, Trial primary completion date:  A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) -  Jun 7, 2023   
    P1,  N=150, Recruiting, 
    Recruiting --> Completed | N=150 --> 40 Trial completion date: Apr 2023 --> Aug 2023 | Trial primary completion date: Apr 2023 --> Aug 2023
  • ||||||||||  PF-07258669 / Pfizer
    Journal:  Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss. (Pubmed Central) -  Mar 11, 2023   
    Introduction of a spirocyclic conformational constraint allowed for simultaneous optimization of MC4R potency and ADME attributes while avoiding the production of hERG active metabolites observed in early series leads. Compound 23 is a potent and selective MC4R antagonist with robust efficacy in an aged rat model of cachexia and has progressed into clinical trials.
  • ||||||||||  PF-07258669 / Pfizer
    Enrollment change:  A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) -  Dec 1, 2022   
    P1,  N=150, Recruiting, 
    This synthetic route consisting of total of 25 synthetic steps (15 linear) delivered API against tight deadlines. N=70 --> 150
  • ||||||||||  PF-07258669 / Pfizer
    Trial completion date, Trial primary completion date:  A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) -  Sep 29, 2022   
    P1,  N=70, Recruiting, 
    N=70 --> 150 Trial completion date: Jul 2022 --> May 2023 | Trial primary completion date: Jul 2022 --> May 2023
  • ||||||||||  PF-07258669 / Pfizer
    Discovery of PF-07258669: A selective and potent small molecule melanocortin-4 receptor antagonist (W183a (McCormick Place Convention Center)) -  Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_11434;    
    Antagonism of MC4R signaling has the potential to mitigate decreased appetite and body weight loss in the setting of anorexia or cachexia due to underlying disease. We will report on the identification of a series of orally bioavailable, small-molecule MC4R antagonists using a focused hit identification effort and the optimization of these antagonists for potency, brain penetration, and ADME attributes leading to the identification of PF-07258669 as a clinical candidate.
  • ||||||||||  PF-07258669 / Pfizer
    Enrollment open:  A Study of PF-07258669 In Healthy Adult Participants (clinicaltrials.gov) -  Jan 4, 2022   
    P1,  N=70, Recruiting, 
    We will report on the identification of a series of orally bioavailable, small-molecule MC4R antagonists using a focused hit identification effort and the optimization of these antagonists for potency, brain penetration, and ADME attributes leading to the identification of PF-07258669 as a clinical candidate. Not yet recruiting --> Recruiting