PF-07054894 / Pfizer - LARVOL DELTA

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=44 | Terminated | Sponsor: Pfizer | Active, not recruiting ➔ Terminated; The study was terminated due to business decision. The decision to terminate the trial was not based on any safety concerns associated with PF-07054894.

Trial termination • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Study to Learn How the Study Medicine Called [14C]PF-07054894 is Processed by the Body (clinicaltrials.gov) - P1 | N=10 | Completed | Sponsor: Pfizer | Active, not recruiting ➔ Completed

Trial completion

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=40 | Active, not recruiting | Sponsor: Pfizer | Recruiting ➔ Active, not recruiting | N=27 ➔ 40

Enrollment change • Enrollment closed • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Discovery of PF-07054894, a Potent Squaramide-Based CCR6 Antagonist Displaying High CXCR2 Selectivity. (PubMed, J Med Chem) - "The mechanism for this effect is rooted in different antagonist-induced ligand-receptor behaviors, insurmountable for CCR6 and surmountable for CXCR2. Herein, we report the discovery and preclinical evaluation of the CCR6 antagonist PF-07054894 (18l) which has advanced to clinical trials as a first in class approach targeting the receptor."

Journal • Immunology • Inflammation • CCL20 • CCR6 • CXCL1 • CXCR2

A Study to Learn How the Study Medicine Called [14C]PF-07054894 is Processed by the Body (clinicaltrials.gov) - P1 | N=10 | Active, not recruiting | Sponsor: Pfizer | Recruiting ➔ Active, not recruiting

Enrollment closed

Enablement and scale up Pfizer's CCR6 and covid-19 (intravenous) assets: Collaborative work between medicinal and process chemistry (ACS-Fall 2025) - "Learnings from the optimization and scale-up synthesis of the squaramide-containing CCR6 lead PF-07054894 are described. Interdepartmental collaborations that were employed to ensure rapid progression will be discussed as well as the final process route and preparation of >7 kg API.The rapid scale up of Lufotrelvir, one of Pfizer's potential Covid-19 anti-viral agents, will also be discussed. Highlights will include the collaboration between the medchem and process groups during the pandemic to simultaneously deliver the toxicology batch and scout for a process friendly clinical development route."

Infectious Disease • Novel Coronavirus Disease • CCR6

A Study to Learn How the Study Medicine Called [14C]PF-07054894 is Processed by the Body (clinicaltrials.gov) - P1 | N=10 | Recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Recruiting

Enrollment open

A Study to Learn How the Study Medicine Called [14C]PF-07054894 is Processed by the Body (clinicaltrials.gov) - P1 | N=10 | Not yet recruiting | Sponsor: Pfizer

New P1 trial

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=27 | Recruiting | Sponsor: Pfizer | Active, not recruiting ➔ Recruiting | N=47 ➔ 27

Enrollment change • Enrollment open • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Study to Learn About the Study Medicine Called PF-07054894 in People of Japanese Origin (clinicaltrials.gov) - P1 | N=6 | Completed | Sponsor: Pfizer | Active, not recruiting ➔ Completed

Trial completion

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=47 | Active, not recruiting | Sponsor: Pfizer | N=29 ➔ 47

Enrollment change • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=29 | Active, not recruiting | Sponsor: Pfizer | Trial completion date: Jul 2024 ➔ Jan 2026 | Trial primary completion date: Jul 2024 ➔ Jan 2026

Trial completion date • Trial primary completion date • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1. (PubMed, ChemMedChem) - "By means of these studies we identified compound 10, a previously reported tert-butyl analogue of navarixin, as a low nanomolar intracellular CCR6 antagonist. Further, our assay platform clearly indicated intracellular binding of the CCR6 antagonist PF-07054894, currently evaluated in phase I clinical trials for the treatment of ulcerative colitis, thereby providing profound evidence for the existence and the pharmacological relevance of a druggable IABS at CCR6."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Oncology • Pulmonary Disease • Respiratory Diseases • Ulcerative Colitis • CCR6 • CXCR1 • CXCR2

A Study to Learn About the Study Medicine Called PF-07054894 in People of Japanese Origin (clinicaltrials.gov) - P1 | N=6 | Active, not recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Active, not recruiting

Enrollment closed

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=29 | Active, not recruiting | Sponsor: Pfizer | Recruiting ➔ Active, not recruiting | Trial completion date: Oct 2024 ➔ Jul 2024 | Trial primary completion date: Oct 2024 ➔ Jul 2024

Enrollment closed • Trial completion date • Trial primary completion date • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Study to Learn About the Study Medicine Called PF-07054894 in People of Japanese Origin (clinicaltrials.gov) - P1 | N=6 | Not yet recruiting | Sponsor: Pfizer

New P1 trial

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1 | N=27 | Recruiting | Sponsor: Pfizer | Phase classification: P1b ➔ P1

Phase classification • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A novel CCR6 antagonist (PF-07054894) that distinguishes between homologous chemokine receptors, increases basal circulating CCR6 T cells, and ameliorates interleukin-23-induced skin inflammation. (PubMed, J Pharmacol Exp Ther) - "PF-07054894 is a novel CCR6 small molecule antagonist that illustrates the importance of binding kinetics in achieving pharmacological potency and selectivity. Orally administered PF-07054894 blocks homeostatic and pathogenic functions of CCR6, suggesting that it is a promising therapeutic agent for the treatment of a variety of autoimmune and inflammatory diseases."

Journal • Dermatitis • Immunology • Inflammation • CCL19 • CCL20 • CCR6 • CCR7 • CXCL1 • CXCR2

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1b | N=27 | Recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Recruiting

Enrollment open • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

A Study to Learn About the Safety, Effects and Pharmacokinetics of Study Medication (PF-07054894) for the Treatment of Ulcerative Colitis (clinicaltrials.gov) - P1b | N=27 | Not yet recruiting | Sponsor: Pfizer

New P1 trial • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Study Of Single And Multiple Ascending Doses Of PF-07054894 In Healthy Adult Participants (clinicaltrials.gov) - P1 | N=84 | Completed | Sponsor: Pfizer | Recruiting ➔ Completed | N=64 ➔ 84

Enrollment change • Trial completion

Study Of Single And Multiple Ascending Doses Of PF-07054894 In Healthy Adult Participants (clinicaltrials.gov) - P1 | N=64 | Recruiting | Sponsor: Pfizer | Trial completion date: Jan 2022 ➔ Jul 2022 | Trial primary completion date: Jan 2022 ➔ Jul 2022

Trial completion date • Trial primary completion date

Study Of Single And Multiple Ascending Doses Of PF-07054894 In Healthy Adult Participants (clinicaltrials.gov) - P1; N=64; Recruiting; Sponsor: Pfizer; Trial completion date: Jun 2021 ➔ Jan 2022; Trial primary completion date: Jun 2021 ➔ Jan 2022

Clinical • Trial completion date • Trial primary completion date

Discovery of the CCR6 antagonist PF-07054894 for the treatment of autoimmune disorders (ACS-Fall 2021) - "Structure-based lead optimization in conjunction with an understanding of differential receptor binding kinetics led to the design of PF-07054894 as a potent, orally bioavailable CCR6 antagonist with high CXCR2 selectivity and efficacy in a pre-clinical model of skin inflammation. This talk will describe the hit to lead effort, SAR driving candidate selection, PK and efficacy in pre-clinical species, and pre-clinical in vitro safety pharmacology that led to the identification of a first-in-class clinical candidate targeting CCR6."

Dermatitis • Dermatology • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Psoriasis • CCL20 • CXCR2

Sosei Heptares Operational Highlights and Consolidated Results for the Nine Months ended 30 September 2020 (PRNewswire) - "Second novel drug candidate resulting from multi-target drug discovery collaboration with Pfizer entered clinical trials – dosing of first subject by Pfizer triggered US$5 million payment to Sosei Heptares. PF-07054894, a CCR6 antagonist targeting Inflammatory Bowel Disease, originating from the Pfizer/Sosei Heptares collaboration, was nominated for clinical development by Pfizer in June 2019."

Commercial • Inflammatory Bowel Disease