RBN-3143 / Ribon Therap - LARVOL DELTA

First-in-Human Phase 1 Study to Evaluate the Clinical Pharmacology Properties of RBN-3143, a Novel Inhibitor of Mono-Adenosine Diphosphate Ribosyltransferase-PARP14. (PubMed, Clin Pharmacol Drug Dev) - "An open-label, randomized, 3-period, cross-over study evaluated the effects of food and pantoprazole (40 mg once daily [QD]) on the pharmacokinetics of RBN-3143 (500 mg), and a pharmacokinetic drug-drug interaction study with oral midazolam (2 mg) determined whether RBN-3143 (300 mg BID for 14 days) is an inducer of cytochrome P4503A4 (CYP3A4). RBN-3143 was an inducer of CYP3A4 in most but not all subjects, with mean midazolam Cmax and AUCinf ratios of 0.92 and 0.88, respectively. The clinical pharmacology properties of RBN-3143 in HVs support further development for inflammatory diseases."

Clinical • Journal • P1 data • Inflammation • Pain • CYP3A4

Discovery and Optimization of Potent and Highly Selective PARP14 Inhibitors for the Treatment of Atopic Dermatitis. (PubMed, J Med Chem) - "Notably, compared to positive control RBN-3143, Q22 showed significant therapeutic efficacy in a dinitrochlorobenzene (DNCB)-induced AD mouse model by markedly reducing the expression of key AD-associated inflammatory cytokines, including IL-4, IL-13, and IL-17A. These findings suggest that Q22 holds considerable promise as a PARP14 inhibitor for AD treatment."

Journal • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Inflammation • IL13 • IL17A • IL4

SAD/MAD Safety and PK Study of RBN-3143 in Healthy and Atopic Dermatitis Subjects (clinicaltrials.gov) - P1 | N=72 | Recruiting | Sponsor: Ribon Therapeutics, Inc. | Trial completion date: Jun 2023 ➔ Sep 2024 | Trial primary completion date: Apr 2023 ➔ Jun 2024

Trial completion date • Trial primary completion date • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • CYP3A4

The PARP14 inhibitor RBN-3143 suppresses skin inflammation in preclinical models (ISID 2023) - P1 | "For all disease features, RBN-3143 either equaled or outperformed treatment with dupilumab. RBN-3143 is well-tolerated in preclinical studies and is the first small molecule inhibitor of PARP14 to enter clinical trials. It is currently being tested in a Phase I study in normal healthy volunteers and patients with atopic dermatitis (NCT05215808)."

IO biomarker • Preclinical • Asthma • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • Inflammation • Pulmonary Disease • Respiratory Diseases • STAT3 • STAT6

Ribon Therapeutics Announces $25 Million Equity Investment from Pfizer (Businesswire) - "Ribon Therapeutics...announced a $25 million investment from Pfizer. Ribon plans to use the proceeds to support clinical development of its potentially first-in-class oral small molecule programs in oncology (RBN-2397, a PARP7 inhibitor) and immunology (RBN-3143, a PARP14 inhibitor)....Separately, Ribon and Pfizer have entered into an agreement to leverage Pfizer’s global development expertise and capabilities to support the advancement of Ribon’s pipeline. Ribon will retain economic rights and control of clinical development across all its programs."

Financing • Licensing / partnership • Immunology • Oncology

Late Breaking Abstract - The PARP14 inhibitor RBN-3143 suppresses lung inflammation in preclinical models (ERS 2022) - P1 | "RBN-3143 is currently in a Phase I clinical trial (NCT05215808) in healthy volunteers. It is the first small molecule inhibitor of PARP14 entering clinical trials and this abstract is the first public disclosure of the compound."

Late-breaking abstract • Preclinical • Asthma • Immunology • Inflammation • Pneumonia • IL33 • IL5 • STAT3 • STAT6 • TSLP

SAD/MAD Safety and PK Study of RBN-3143 in Healthy and Atopic Dermatitis Subjects (clinicaltrials.gov) - P1 | N=72 | Recruiting | Sponsor: Ribon Therapeutics, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Atopic Dermatitis • Dermatitis • Dermatology • Immunology • CYP3A4