SMP-100 / Chengdu Kelingyuan Pharma, ConSynance, Curia - LARVOL DELTA

Structural basis for partial agonism in 5-HT receptors. (PubMed, Nat Struct Mol Biol) - "Here, we present high-resolution cryogenic electron microscopy structures of the mouse 5-HTR in complex with partial agonists (SMP-100 and ALB-148471) captured in pre-activated and open-like conformational states. Molecular dynamics simulations were used to assess the stability of drug-binding poses and interactions with the receptor over time. Together, these studies reveal mechanisms for the functional differences between orthosteric partial agonists, full agonists and antagonists of the 5-HTR."

Journal • Chemotherapy-Induced Nausea and Vomiting • Gastrointestinal Disorder

A Phase 1 Study of SMP-100 in Normal Healthy Volunteers (clinicaltrials.gov) - P1 | N=53 | Completed | Sponsor: Chengdu SciMount Pharmatech Co., Ltd. | Active, not recruiting ➔ Completed | Trial completion date: Apr 2022 ➔ Aug 2021 | Trial primary completion date: Feb 2022 ➔ Jul 2021

Trial completion • Trial completion date • Trial primary completion date

3-Way Crossover Study to Compare the PK (Pharmokinetics) and to Evaluate the Effect of Food on the Bioavailability (clinicaltrials.gov) - P1 | N=8 | Completed | Sponsor: Chengdu SciMount Pharmatech Co., Ltd. | Recruiting ➔ Completed | N=12 ➔ 8 | Trial completion date: Mar 2022 ➔ Dec 2021

Enrollment change • Trial completion • Trial completion date

A Phase 1 Study of SMP-100 in Normal Healthy Volunteers (clinicaltrials.gov) - P1; N=72; Active, not recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.; Trial completion date: Oct 2021 ➔ Apr 2022; Trial primary completion date: Aug 2021 ➔ Feb 2022

Clinical • Trial completion date • Trial primary completion date

3-Way Crossover Study to Compare the PK (Pharmokinetics) and to Evaluate the Effect of Food on the Bioavailability (clinicaltrials.gov) - P1; N=12; Recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open

3-Way Crossover Study to Compare the PK (Pharmokinetics) and to Evaluate the Effect of Food on the Bioavailability (clinicaltrials.gov) - P1; N=12; Not yet recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.

Clinical • New P1 trial

A Phase 1 Study of SMP-100 in Normal Healthy Volunteers (clinicaltrials.gov) - P1; N=72; Active, not recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.; Recruiting ➔ Active, not recruiting

Enrollment closed

CSTI-300; a novel 5-HT receptor partial agonist with potential to treat patients with irritable bowel syndrome or carcinoid syndrome. (PubMed, J Pharmacol Exp Ther) - "SIGNIFICANCE STATEMENT: There is a lack of effective current treatment for IBS-d and carcinoid syndrome, and in both conditions, over-activity of the 5-HT receptor is thought to be implicated in the pathophysiology. As 5-HT receptor blockade with antagonists results in significant side effects, we present evidence that treatment with a suitable 5-HT receptor partial agonist will alleviate some symptoms associated with these conditions yet without fully inhibiting the receptor predict a less pronounced side effect profile associated with this therapeutic strategy."

Clinical • Journal • Carcinoid Tumor • Constipation • Immunology

A Phase 1 Study of SMP-100 in Normal Healthy Volunteers (clinicaltrials.gov) - P1; N=72; Recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.; Not yet recruiting ➔ Recruiting; Trial completion date: Mar 2021 ➔ Jul 2021; Trial primary completion date: Nov 2020 ➔ Apr 2021

Clinical • Enrollment open • Trial completion date • Trial primary completion date • Reperfusion Injury

A Phase 1 Study of SMP-100 in Normal Healthy Volunteers (clinicaltrials.gov) - P1; N=72; Not yet recruiting; Sponsor: Chengdu SciMount Pharmatech Co., Ltd.

Clinical • New P1 trial