sitokiren (SPH3127) / Shanghai Pharma - LARVOL DELTA

A Study of SPH3127 in the Treatment of Mild to Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=53 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Recruiting ➔ Completed | N=108 ➔ 53 | Trial completion date: Dec 2025 ➔ Sep 2024 | Trial primary completion date: Dec 2025 ➔ Sep 2024

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

Evaluation of SPH3127 in Patients With Mild-to-Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=3 | Terminated | Sponsor: Shanghai Pharma Biotherapeutics USA Inc. | N=30 ➔ 3 | Recruiting ➔ Terminated; Shanghai Pharma Biotherapeutics USA Inc. experienced difficulty in recruiting clinical research sites and in enrolling patients with ulcerative colitis, and consequently, the study was terminated due to futility.

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

SPH3127 (Sitokiren), a Novel Renin Inhibitor, Suppresses Colitis Development in Mouse Models of Experimental Colitis. (PubMed, Inflamm Bowel Dis) - "These results demonstrate that SPH3127 is able to effectively block colitis development in mouse experimental colitis models. Its anti-colitogenic activity is achieved at least in part by suppressing mucosal TH1 and TH17 activation while promoting IL-10 production from mucosal CD25+ T cells, thus forming an anti-inflammatory environment in the colonic mucosa."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • IFNG • IL10 • IL17A • IL1B • IL2RA • IL6 • TNFA

Shanghai Pharmaceuticals: The application for marketing authorization of SPH3127 tablets has been accepted [Google translation] (China United International) - "Shanghai Pharmaceuticals: The application for marketing authorization of SPH3127 tablets has been accepted."

China filing • Inflammatory Bowel Disease

A Study of SPH3127 in the Treatment of Mild to Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=108 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial completion date: Feb 2025 ➔ Dec 2025 | Trial primary completion date: Feb 2025 ➔ Dec 2025

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

Efficacy and Safety of SPH3127 Tablets on Treating the Diabetic Kidney Disease (clinicaltrials.gov) - P2 | N=305 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial completion date: Jun 2025 ➔ Dec 2024 | Recruiting ➔ Completed | Trial primary completion date: Jun 2025 ➔ Dec 2024

Trial completion • Trial completion date • Trial primary completion date • Diabetic Nephropathy • Nephrology • Renal Disease • EGFR

Efficacy and Safety of SPH3127 Tablets on Treating the Diabetic Kidney Disease (clinicaltrials.gov) - P2 | N=320 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial completion date: Mar 2025 ➔ Jun 2025 | Trial primary completion date: Sep 2024 ➔ Jun 2025

Trial completion date • Trial primary completion date • Diabetic Nephropathy • Nephrology • Renal Disease • EGFR

SPH3127-301: Study to Evaluate the Efficacy and Safety of SPH3127 In Patients With Mild-moderate Essential Hypertension (clinicaltrials.gov) - P3 | N=957 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Recruiting ➔ Completed | Trial completion date: Apr 2024 ➔ Dec 2023 | Trial primary completion date: Mar 2024 ➔ Dec 2023

Trial completion • Trial completion date • Trial primary completion date • Cardiovascular • Hypertension

A randomized, double-blind, placebo-controlled, phase IIa, clinical study on investigating the efficacy and safety of SPH3127 tablet in patients with essential hypertension. (PubMed, Hypertens Res) - P2 | "SPH3127 is a promising drug for the treatment of patients with essential hypertension. The recommended dosage is 100 mg daily.Clinical trial registration: This study was registered in ClinicalTrials.gov (NCT03756103)."

Clinical • Journal • P2a data • Cardiovascular • Hypertension

SPH3127-301: Study to Evaluate the Efficacy and Safety of SPH3127 In Patients With Mild-moderate Essential Hypertension (clinicaltrials.gov) - P3 | N=900 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial primary completion date: Oct 2023 ➔ Mar 2024

Trial primary completion date • Cardiovascular • Hypertension

Evaluation of SPH3127 in Patients With Mild-to-Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Shanghai Pharma Biotherapeutics USA Inc. | Trial completion date: Apr 2024 ➔ Dec 2025

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

SPH3127-301: Study to Evaluate the Efficacy and Safety of SPH3127 In Patients With Mild-moderate Essential Hypertension (clinicaltrials.gov) - P3 | N=900 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial primary completion date: May 2023 ➔ Oct 2023

Trial primary completion date • Cardiovascular • Hypertension

A Study of SPH3127 in the Treatment of Mild to Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=108 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Not yet recruiting ➔ Recruiting

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

Efficacy and Safety of SPH3127 Tablets on Treating the Diabetic Kidney Disease (clinicaltrials.gov) - P2 | N=320 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Diabetic Nephropathy • Nephrology • Renal Disease • EGFR

A Study of SPH3127 in the Treatment of Mild to Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=108 | Not yet recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P2 trial • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Study on Human Mass Balance of SPH3127 Tablets (clinicaltrials.gov) - P1/2 | N=6 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Active, not recruiting ➔ Completed | Trial completion date: Feb 2023 ➔ Oct 2022

Trial completion • Trial completion date • Cardiovascular • Hypertension

Study on Human Mass Balance of SPH3127 Tablets (clinicaltrials.gov) - P1/2 | N=6 | Active, not recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Recruiting ➔ Active, not recruiting

Enrollment closed • Cardiovascular • Hypertension

Efficacy and Safety of SPH3127 Tablets on Treating the Diabetic Kidney Disease (clinicaltrials.gov) - P2 | N=320 | Not yet recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P2 trial • Diabetic Nephropathy • Nephrology • Renal Disease • EGFR

Study on Human Mass Balance of SPH3127 Tablets (clinicaltrials.gov) - P1/2 | N=6 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P1/2 trial • Cardiovascular • Hypertension

Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor. (PubMed, J Med Chem) - "Therefore, we tried to find nonpeptidomimetic DRIs with a MW of < 500 and discovered the promising 2-carbamoyl morpholine derivative 4. In our efforts to improve the pharmacokinetic profile of 4 without a significant increase in the MW, we discovered compound 18 (SPH3127), which demonstrated higher bioavailability and a more potent antihypertensive effect in preclinical models than aliskiren and has completed a phase II clinical trial for essential hypertension."

Journal • Cardiovascular • Hypertension • Nephrology • Renal Disease

SPH3127-104: Drug-drug Interaction Study of SPH3127 (clinicaltrials.gov) - P1/2 | N=40 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Active, not recruiting ➔ Completed | Trial completion date: Jun 2022 ➔ Jan 2022 | Trial primary completion date: Apr 2022 ➔ Jan 2022

Trial completion • Trial completion date • Trial primary completion date

Study to Evaluate the Efficacy and Safety of SPH3127 In Patients With Mild-moderate Essential Hypertension (clinicaltrials.gov) - P3 | N=900 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P3 trial • Hypertension

Drug-drug Interaction Study of SPH3127 (clinicaltrials.gov) - P1/2 | N=40 | Active, not recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P1/2 trial

Evaluation of SPH3127 in Patients With Mild-to-Moderate Ulcerative Colitis (clinicaltrials.gov) - P2 | N=30 | Recruiting | Sponsor: Shanghai Pharma Biotherapeutics USA Inc. | Initiation date: Sep 2021 ➔ Mar 2022

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

The Tolerability and Pharmacokinetics of Multiple Doses of SPH3127 in Chinese Healthy People (clinicaltrials.gov) - P1; N=24; Completed; Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd; Recruiting ➔ Completed

Clinical • Trial completion • Hypertension