Delving into the Latest Updates on Insilico Medicine Shanghai Ltd with Synapse

Overview

Basic Info

Introduction

InSilico Medicine (Shanghai) Ltd. was established on June 13, 2019. InSilico Medicine is a clinical-stage biopharmaceutical company powered by end-to-end artificial intelligence. The company focuses on unmet medical needs in areas such as cancer, fibrosis, immunity, central nervous system disorders, and age-related diseases, pushing forward and accelerating the development of innovative drugs.

Tags

Neoplasms

Digestive System Disorders

Respiratory Diseases

Small molecule drug

Chemical drugs

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	20
Immune System Diseases	4
Nervous System Diseases	2
Hemic and Lymphatic Diseases	2
Endocrinology and Metabolic Disease	2
Infectious Diseases	1

Top 5 Drug Type	Count

Small molecule drug	22
Chemical drugs	4

Top 5 Target	Count

POLQ(DNA polymerase theta)	2
WRN(WRN RecQ like helicase)	2
CDK7(Cyclin-dependent kinase 7)	2
MYT1(myelin transcription factor 1)	1
QPCTL(glutaminyl-peptide cyclotransferase like)	1

本试验主要目的旨在评价ISM6331在晚期或转移性恶性间皮瘤或其他实体瘤受试者中的安全性和耐受性和确定II期推荐剂量。本试验次要目的为评价ISM6331单次和多次给药后血浆中ISM6331的药代动力学（PK）特征以及评价ISM6331单药治疗的初步疗效。本试验探索性目的为评价ISM6331的药效动力学（PD）效应和潜在预测性生物标志物，并探索ISM6331的代谢产物。

[Translation]

The primary purpose of this trial is to evaluate the safety and tolerability of ISM6331 in subjects with advanced or metastatic malignant mesothelioma or other solid tumors and to determine the recommended dose for Phase II. The secondary purpose of this trial is to evaluate the pharmacokinetic (PK) characteristics of ISM6331 in plasma after single and multiple doses of ISM6331 and to evaluate the preliminary efficacy of ISM6331 monotherapy. The exploratory purpose of this trial is to evaluate the pharmacodynamic (PD) effects and potential predictive biomarkers of ISM6331 and to explore the metabolites of ISM6331.

Start Date12 Dec 2024

Sponsor / Collaborator

Insilico Medicine Shanghai Ltd

CTR20241789

/ CompletedPhase 1

一项随机、双盲、安慰剂对照的单次、多次给药剂量递增研究以及食物影响研究以评估ISM5411在中国健康受试者中的安全性、耐受性、药代动力学特征和食物影响

[Translation] A randomized, double-blind, placebo-controlled single-dose, multiple-dose ascending study and food effect study to evaluate the safety, tolerability, pharmacokinetic characteristics and food effect of ISM5411 in healthy Chinese subjects

主要目的：评估ISM5411单次和多次口服给药在中国健康受试者中的安全性和耐受性。次要目的：评估ISM5411单次和多次口服给药后，ISM5411和M15（ISM5411代谢物）在中国健康受试者中的药代动力学（Pharmacokinetics，PK）特征。评估食物在中国健康受试者单次服用ISM5411后，对ISM5411和M15（ISM5411代谢物）PK特性的影响。探索性目的：评估ISM5411单次和多次口服给药后，中国健康受试者外周血生物标志物（促红细胞生成素和血管内皮生长因子）和粪便生物标志物（钙卫蛋白和脂质运载蛋白-2）的表达变化。

[Translation]

Primary objectives: To evaluate the safety and tolerability of single and multiple oral administration of ISM5411 in healthy Chinese subjects. Secondary objectives: To evaluate the pharmacokinetic (PK) characteristics of ISM5411 and M15 (metabolite of ISM5411) in healthy Chinese subjects after single and multiple oral administration of ISM5411. To evaluate the effect of food on the PK characteristics of ISM5411 and M15 (metabolite of ISM5411) after a single dose of ISM5411 in healthy Chinese subjects. Exploratory objectives: To evaluate the changes in the expression of peripheral blood biomarkers (erythropoietin and vascular endothelial growth factor) and fecal biomarkers (calprotectin and lipocalin-2) in healthy Chinese subjects after single and multiple oral administration of ISM5411.

Start Date26 May 2024

Sponsor / Collaborator

Insilico Medicine Shanghai Ltd

CTR20240727

/ RecruitingPhase 1

一项评价ISM8207治疗晚期实体瘤和复发/难治性B细胞淋巴瘤受试者的安全性、耐受性、药代动力学和初步疗效的I期、开放性、多中心、首次人体研究

[Translation] A Phase I, open-label, multicenter, first-in-human study to evaluate the safety, tolerability, pharmacokinetics, and preliminary efficacy of ISM8207 in subjects with advanced solid tumors and relapsed/refractory B-cell lymphoma

本试验主要目的旨在评价ISM8207治疗晚期实体瘤和复发/难治性B细胞淋巴瘤受试者的安全性和耐受性和确定ISM8207治疗晚期实体瘤和R/R B细胞淋巴瘤受试者的II期推荐剂量。本试验次要目的为评价ISM8207治疗晚期实体瘤和R/R B细胞淋巴瘤受试者的初步临床疗效以及评估ISM8207单次及多次给药后的药代动力学特征。本试验探索性目的为探索ISM8207的代谢物和评价ISM8207的药效动力学特征。

[Translation]

The primary purpose of this trial is to evaluate the safety and tolerability of ISM8207 in the treatment of subjects with advanced solid tumors and relapsed/refractory B-cell lymphoma and to determine the recommended Phase II dose of ISM8207 in the treatment of subjects with advanced solid tumors and R/R B-cell lymphoma. The secondary purpose of this trial is to evaluate the preliminary clinical efficacy of ISM8207 in the treatment of subjects with advanced solid tumors and R/R B-cell lymphoma and to evaluate the pharmacokinetic characteristics of ISM8207 after single and multiple administrations. The exploratory purpose of this trial is to explore the metabolites of ISM8207 and evaluate the pharmacodynamic characteristics of ISM8207.

Start Date11 Apr 2024

Sponsor / Collaborator

Insilico Medicine Shanghai Ltd

100 Clinical Results associated with Insilico Medicine Shanghai Ltd

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0 Patents (Medical) associated with Insilico Medicine Shanghai Ltd

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30

Literatures (Medical) associated with Insilico Medicine Shanghai Ltd

24 Apr 2025·Journal of Medicinal Chemistry

Discovery of WEE1 Kinase Inhibitors with Potent Activity against Patient-Derived, Metastatic Colorectal Cancer Organoids

Article

Author: Mukherjee, Siddhartha ; Woods, Susan L. ; Wang, Xiaomin ; Zhavoronkov, Alex ; Chang, Aeson ; Fenix, Kevin ; Barratt, Kate ; Wei, Heping ; Ramsay, Robert G. ; Gee, Yi Sing ; Heriot, Alexander ; Tin, Teresa ; Sammour, Tarik ; Lawrence, Matthew J. ; Posch, Markus ; Lu, Hongfu ; de Nys, Rebekah ; Syphers, Joel L. ; Huang, Fei ; Baell, Jonathan B. ; Liu, Shen ; Narasimhan, Vignesh ; Che, Da Qing ; Wright, Josephine A. ; Vrbanac, Laura ; Silva, Tharindie N. ; Maddern, Guy J. ; Priebbenow, Daniel L. ; Sloan, Erica K. ; Kelter, Gerhard ; Worthley, Daniel L. ; Gao, Fan ; Maier, Armin ; Mudududdla, Ramesh ; Kaur, Harleen

A library of potent WEE1 kinase inhibitors was synthesized based on the discontinued frontrunner clinical candidate AZD1775 (1), many of which were more selective for WEE1 over an undesirable off-target of 1, the kinase PLK1. When tested against patient-derived organoids (PDOs) grown from TP53-mutated colorectal cancer (CRC) peritoneal metastases, 34 (IC₅₀ value of 62 nM) exhibited stronger efficacy than 1 (IC₅₀ value of 120 nM) and the best-in-class clinical candidate ZN-c3 (IC₅₀ value of 127 nM). Against primary CRC PDOs with TP53-WT, 34 significantly enhanced DNA damage, replication stress and apoptosis compared to 1, as well as demonstrated high selectivity over patient-matched normal healthy colon PDOs, highlighting a potential therapeutic window for cancer treatment. Overall, this investigation provides critical insight into several potent WEE1 inhibitors that exhibited exceptional efficacy against CRC PDOs and is the first to utilize a PDO platform to assess their effect on healthy and malignant cell viability.

10 Apr 2025·Journal of Medicinal Chemistry

Discovery of Novel SIK2/3 Inhibitors for the Potential Treatment of MEF2C+ Acute Myeloid Leukemia (AML)

Article

Author: Gao, Feng ; Zhu, Wei ; Zhavoronkov, Alex ; Aliper, Alex ; Cai, Xin ; Zhang, Man ; Liu, Tingting ; Ding, Xiao ; Li, Qi ; Zhao, Pei ; Ren, Feng

The dual inhibition of SIK2/3 has been considered as a potential treatment approach for MEF2C-high acute myeloid leukemia (AML). Although diverse scaffolds of pan-SIK or SIK2/3 inhibitors have been reported, few of them showed sufficient in vitro or in vivo antitumor activity. Based on the proposed binding mode of the hit molecule (7), chemical space in the solvent/P-loop region was explored via fragment growing/replacement, supported by the generative chemistry platform. Further SAR exploration and ADME optimization led to the discovery of 7s, which exhibited excellent potency and strong selectivity in MEF2C high-expression cell lines over MEF2C-low cell lines. Moreover, oral administration of 7s was found to demonstrate significant tumor growth inhibition in a MV4-11 AML mice CDX model without any body weight loss. This work highlights the potential of targeting MEF2C-dependent AML by selective oral SIK2/3 inhibitors, which was supported by the generative models.

27 Feb 2025·Journal of Medicinal Chemistry

Design, Synthesis, and Biological Evaluation of Novel Orally Available Covalent CDK12/13 Dual Inhibitors for the Treatment of Tumors

Article

Author: Aliper, Alex ; Sun, Deheng ; Wu, Jianping ; Wang, Zhen ; Zhang, Haoyu ; Ding, Xiao ; Zhavoronkov, Alex ; Cai, Xin ; Cui, Hui ; Min, Lihua ; Zhang, Yihong ; Ren, Feng ; Lu, Hongfu ; Zhang, Man

Cyclin-dependent kinases 12 and 13 (CDK12/13) safeguard genomic integrity by preferentially regulating gene expression in the DNA damage response (DDR). The CDK12/13-mediated upregulation of DDR genes and pathways significantly contributes to both tumorigenesis and the development of resistance to antitumor therapies. Thus, the functional inhibition of CDK12/13 offers an attractive strategy to combat carcinogenesis, particularly for refractory and treatment-resistant cancers. Here, we report the discovery of compound 12b as a novel, potent, orally available covalent CDK12/13 dual inhibitor with a promising safety profile and robust in vivo antitumor properties.

100 Deals associated with Insilico Medicine Shanghai Ltd

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100 Translational Medicine associated with Insilico Medicine Shanghai Ltd

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Pipeline

Pipeline Snapshot as of 10 May 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Discovery

9

11

Preclinical

IND Approval

2

5

Phase 1 Clinical

Phase 2 Clinical

1

Other

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Rentosertib ( TNIK )	Idiopathic Pulmonary Fibrosis More	Phase 2
ISM-3312 ( SARS-CoV-2 3CLpro )	COVID-19 More	Phase 1
ISM-5411 ( EGLN2 x PHD2 )	Inflammatory Bowel Diseases More	Phase 1
ISM-6331 ( TEAD )	Solid tumor More	Phase 1
ISM-8207 ( QPCTL )	B-cell lymphoma refractory More	Phase 1