Delving into the Latest Updates on SIPI-7623 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

FXR

Mechanism

FXR antagonists(Bile acid receptor FXR antagonists)

Therapeutic Areas

Congenital DisordersEndocrinology and Metabolic Disease

Active Indication-

Inactive Indication

HypercholesterolemiaHyperlipidemia, Familial Combined

Originator Organization

Nanjing Carephar Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Shanghai Institute of Pharmaceutical Industry

Jiangsu Carephar Pharmaceutical Co., Ltd.

Nanjing Carephar Pharmaceutical Co., Ltd.

Drug Highest PhaseSuspendedPhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC23H29NO4

InChIKeyJEQWMSZFVYEBQQ-UHFFFAOYSA-N

CAS Registry1416548-73-6

Primary purpose: To explore the safety of hyperlipidemic subjects after multiple administration of SIPI-7623 tablets. Secondary purpose: To explore the pharmacokinetic characteristics and drug effects of hyperlipidemic subjects after multiple administration of SIPI-7623 tablets, and to provide a basis for the formulation of Phase II clinical trial plan.

Start Date07 Oct 2019

Sponsor / Collaborator

Shanghai Institute of Pharmaceutical Industry

[+1]

CTR20182217 / SuspendedPhase 1

SIPI-7623片在健康受试者中随机双盲、安慰剂对照、单剂量耐受性、进食影响与药代动力学临床试验

[Translation] A randomized, double-blind, placebo-controlled, single-dose clinical trial of SIPI-7623 tablets in healthy subjects to evaluate tolerance, effect of food intake, and pharmacokinetics

评价SIPI-7623片单次给药在健康受试者中的安全性、耐受性、食物影响以及药代动力学特征。

[Translation]

To evaluate the safety, tolerability, food effect, and pharmacokinetic characteristics of a single dose of SIPI-7623 tablets in healthy subjects.

Start Date21 Feb 2019

Sponsor / Collaborator

Shanghai Institute of Pharmaceutical Industry

[+1]

100 Clinical Results associated with SIPI-7623

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100 Translational Medicine associated with SIPI-7623

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100 Patents (Medical) associated with SIPI-7623

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2

Literatures (Medical) associated with SIPI-7623

01 Feb 2019·Molecular DiversityQ3 · CHEMISTRY

Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists

Q3 · CHEMISTRY

Article

Author: Zhou, Yi-Huan ; Wang, Guo-Ping ; Nian, Si-Yun ; Tan, Xiang-Duan ; Xiao, Ying ; Huang, Mo-Han ; Jiang, Zheng-Li

Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC₅₀ = 7.8 ± 1.1 μM) showed better activity compared to SIPI-7623 (IC₅₀ = 40.8 ± 1.7 μM) and guggulsterone (IC₅₀ = 45.9 ± 1.1 μM). Docking of A-11 in FXR's ligand-binding domain was also studied.

01 Aug 2018·Chinese Journal of Natural MedicinesQ2 · MEDICINE

Hypolipidemic effect of SIPI-7623, a derivative of an extract from oriental wormwood, through farnesoid X receptor antagonism

Q2 · MEDICINE

Article

Author: Yu, Peng-Xia ; Liu, Min-Yu ; Huang, Xiao-Ling ; Zhang, Zhen ; Liu, Quan-Hai ; Su, Mei ; Deng, Yi-Fang ; Wang, Guo-Ping

Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily of ligand-activated transcription factors. As a metabolic regulator, FXR plays key roles in bile acid and cholesterol metabolism and lipid and glucose homeostasis. Therefore, FXR is a potential drug target for several metabolic syndromes, especially those related to lipidemia disorders. In the present study, we identified small molecule SIPI-7623, a derivative of an extract from Oriental wormwood (Artemisia capillaris), and found that it specifically upregulated the expression of cholesterol-7-alpha-hydroxylase (CYP7A1), downregulated the expression of sterol-regulatory element-binding protein 1c (SREBP-1c) in the liver, and inhibited the expression of ileal bile acid binding-protein (IBABP) in the ileum of rats. We found that inhibition of FXR by SIPI-7623 decreased the level of cholesterol and triglyceride. SIPI-7623 reduced the levels of cholesterol and triglyceride in in vitro HepG2 cell models, ameliorated diet-induced atherosclerosis, and decreased the serum lipid content on rats and rabbits model of atherosclerosis in vivo. Furthermore, SIPI-7623 decreased the extent of atherosclerotic lesions. Our resutls demonstrated that antagonism of the FXR pathway can be employed as a therapeutic strategy to treat metabolic diseases such as hyperlipidemia and atherosclerosis. In conclusion, SIPI-7623 could be a promising lead compound for development of drugs to treat hyperlipidemia and atherosclerosis.

100 Deals associated with SIPI-7623

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypercholesterolemia	Phase 1	CN	Jiangsu Carephar Pharmaceutical Co., Ltd.	26 Sep 2021
Hyperlipidemia, Familial Combined	Phase 1	CN	Shanghai Institute of Pharmaceutical Industry	21 Feb 2019
Hyperlipidemia, Familial Combined	Phase 1	CN	Nanjing Carephar Pharmaceutical Co., Ltd.	21 Feb 2019