Top 5 Target	Count

EZH2(Histone-lysine N-methyltransferase EZH2)	2
5-HT receptor(Serotonin (5-HT) receptor)	1
BTK(Tyrosine-protein kinase BTK)	1
TYK2(Tyrosine-protein kinase 2)	1
μ opioid receptor(Mu opioid receptor)	1

Drugs associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

HHT120

Target

thrombin

Mechanism

thrombin inhibitors

Active Org.

Livzon Pharmaceutical Group, Inc. [+1]

Originator Org.

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

Active Indication

Venous Thromboembolism [+1]

Inactive Indication-

Drug Highest PhasePhase 1

First Approval Ctry. / Loc.-

First Approval Date-

HHT-109

Target

JAK1

Mechanism

JAK1 inhibitors

Active Org.

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

Originator Org.

Zhejiang Huahai Pharmaceutical Co., Ltd.

Active Indication

Rheumatoid Arthritis

Inactive Indication-

Drug Highest PhaseIND Approval

First Approval Ctry. / Loc.-

First Approval Date-

EZH2 Inhibitor(Synergy Pharmaceutical)

Target

EZH2

Mechanism

EZH2 inhibitors

Active Org.

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

Originator Org.

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

Active Indication

Lymphoma

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date-

Clinical Trials associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

CTR20241234 / RecruitingPhase 1

评价HHT201（注射用双羟萘酸多奈哌齐）在健康受试者中的安全性、耐受性及药代动力学特征的单中心、开放标签、单剂量递增的Ⅰ期临床研究

[Translation] A single-center, open-label, single-dose escalation phase I clinical study to evaluate the safety, tolerability and pharmacokinetic characteristics of HHT201 (donepezil pamoate for injection) in healthy subjects

主要研究目的：评价HHT201在健康受试者中的安全性和耐受性；次要研究目的：HHT201在健康受试者的药代动力学（PK）特征。

[Translation]

Primary study objective: To evaluate the safety and tolerability of HHT201 in healthy subjects; Secondary study objective: To investigate the pharmacokinetic (PK) characteristics of HHT201 in healthy subjects.

Start Date05 Jun 2024

Sponsor / Collaborator

Zhejiang Huahai Pharmaceutical Co., Ltd.

[+1]

NCT06373094 / Not yet recruitingPhase 1

A Single-center, Open-label, Single-dose Ascending Phase I Clinical Study Evaluating the Safety, Tolerability, and Pharmacokinetic Profile of HHT201 (Donepezil Dihydroxynaphthalate for Injection) in Healthy Subjects

The objective of this study is to evaluate the safety and pharmacokinetic profiles of HHT201 in healthy subjects.

Start Date01 Jun 2024

Sponsor / Collaborator

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

CTR20221837 / RecruitingPhase 1

一项评价HHT120胶囊在健康受试者中的安全性、耐受性、药代动力学及药效动力学特征的单次、多次给药剂量递增及食物对PK影响的I期临床研究

[Translation] A Phase I clinical study to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic characteristics of HHT120 capsules in healthy subjects with single and multiple dose escalation and the effect of food on PK

主要研究目的：评价健康受试者单次及多次服用HHT120胶囊后的安全性、耐受性。次要研究目的：评价健康受试者单次及多次服用HHT120胶囊后的药代动力学特征；评价健康受试者单次及多次服用HHT120胶囊后的药效动力学特征；评价健康受试者单次及多次服用HHT120胶囊后血药浓度与药效动力学的相关性；评价健康受试者空腹及餐后状态下服用HHT120胶囊的药代动力学特征，评价食物对药代动力学特征的影响。探索性目的：健康受试者单次服用HHT120胶囊后人体内的主要代谢产物鉴定；健康受试者单次及多次服用HHT120胶囊后对QT间期的影响。

[Translation]

Main research objectives: Evaluate the safety and tolerability of HHT120 capsules after single and multiple doses in healthy subjects. Secondary research objectives: Evaluate the pharmacokinetic characteristics of HHT120 capsules after single and multiple doses in healthy subjects; Evaluate the pharmacodynamic characteristics of HHT120 capsules after single and multiple doses in healthy subjects; Evaluate the correlation between blood drug concentration and pharmacodynamics after single and multiple doses of HHT120 capsules in healthy subjects; Evaluate the pharmacokinetic characteristics of HHT120 capsules in healthy subjects in fasting and postprandial states, and evaluate the effect of food on pharmacokinetic characteristics. Exploratory objectives: Identification of the main metabolites in the human body after a single dose of HHT120 capsules in healthy subjects; The effect of single and multiple doses of HHT120 capsules on the QT interval in healthy subjects.

Start Date29 Jan 2024

Sponsor / Collaborator

Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

100 Clinical Results associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

0 Patents (Medical) associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

Literatures (Medical) associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

01 Jan 2024·Bioorganic & Medicinal Chemistry Letters

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

Article

Author: Zhang, Xiaojuan ; Chen, Jia ; Li, Min ; Guo, Fengying ; Zhou, Xiaobo ; Wang, Guan ; Xu, Xin ; Li, Qiang

The enhancer of zeste homolog 2 (EZH2) plays the role of the main catalytic subunit of polycomb repressive complex 2 (PRC2) that catalyzes the methylation of histone H3 lysine 27 (H3K27). Overexpression or mutation of EZH2 has been observed in many types of hematologic malignancies and solid tumors, such as myeloma, lymphoma, prostate, breast, kidney, and lung cancers. EZH2 has been demonstrated as a promising therapeutic target for the treatment of tumors. Based on the structure of 1 (EPZ-6438), a series of novel conformationally constrained derivatives were designed and synthesized aiming to improve the EZH2 inhibition activity, especially for mutated EZH2. Structure and activity relationship (SAR) exploration and optimization at both enzymatic and cellular levels led to the discovery of 28. In vitro, 28 displayed potent EZH2 inhibition activity with an IC₅₀ value of 0.95 nM, which is comparable to EPZ-6438 (1). 28 exhibited high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC₅₀ = 2.36, 1.73, and 1.82 nM, respectively). In vivo, 28 showed acceptable pharmacokinetic characteristics (oral bioavailability F = 36.9%) and better efficacy than 1 in both Pfeiffer and Karpas-422 xenograft mouse models, suggesting that it can be further developed as a potential therapeutic candidate for EZH2-associated cancers.

01 Jan 2021·Analytical BiochemistryQ4 · BIOLOGY

Optimizations of a novel fluorescence polarization-based high-throughput screening assay for β-catenin/LEF1 interaction inhibitors

Q4 · BIOLOGY

Article

Author: Liu, Xiaoping ; Yue, Yuhuan ; Chen, Yunyu ; Li, Dongsheng ; Fu, Zhenghao

Aberrant activation of the Wnt/β-catenin signaling pathway is prominent in the development and metastasis of non-small cell lung cancer (NSCLC). Highly effective inhibition of this pathway highlights a therapeutic avenue against NSCLC. Moreover, β-catenin/LEF1 interaction regulates β-catenin nuclear transport as well as the transcriptions of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, interruption of this interaction would be a promising therapeutic strategy for NSCLC metastasis. To date, no economical and rapid high-throughput screening (HTS) assay has been reported for the discovery of β-catenin/LEF1 interaction inhibitors. In this study, we developed a novel fluorescence polarization (FP)-based HTS assay to identify β-catenin/LEF1 interaction inhibitors. The FITC-LEF1 sequence, incubation time, temperature, and DMSO resistance were optimized, and then a high Z' factor of 0.77 was achieved. A pilot screening of a natural product library via this established FP screening assay identified sanguinarine analogues as potential β-catenin/LEF1 interaction inhibitors. GST pull-down and surface plasmon resonance (SPR) assay demonstrated that β-catenin/LEF1 interaction is a potential anticancer target of sanguinarine in vitro. This newly developed FP screening assay will be vital for the rapid discovery of novel Wnt inhibitors targeting β-catenin/LEF1 interaction.

Bioorganic & Medicinal Chemistry Letters

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

Author: Zhou, Xiaobo ; Li, Min ; Li, Qiang ; Wang, Guan ; Chen, Jia ; Xu, Xin ; Zhang, Xiaojuan ; Guo, Fengying

The enhancer of zeste homolog 2 (EZH2) plays the role of the main catalytic subunit of polycomb repressive complex 2 (PRC2) that catalyzes the methylation of histone H3 lysine 27 (H3K27).Overexpression or mutation of EZH2 has been observed in many types of hematol. malignancies and solid tumors, such as myeloma, lymphoma, prostate, breast, kidney, and lung cancers.EZH2 has been demonstrated as a promising therapeutic target for the treatment of tumors.Based on the structure of 1 (EPZ-6438), a series of novel conformationally constrained derivatives were designed and synthesized aiming to improve the EZH2 inhibition activity, especially for mutated EZH2.Structure and activity relationship (SAR) exploration and optimization at both enzymic and cellular levels led to the discovery of 28.In vitro, 28 displayed potent EZH2 inhibition activity with an IC50 value of 0.95 nM, which is comparable to EPZ-6438 (1). 28 exhibited high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 = 2.36, 1.73, and 1.82 nM, resp.). In vivo, 28 showed acceptable pharmacokinetic characteristics (oral bioavailability F = 36.9%) and better efficacy than 1 in both Pfeiffer and Karpas-422 xenograft mouse models, suggesting that it can be further developed as a potential therapeutic candidate for EZH2-associated cancers.

100 Deals associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

100 Translational Medicine associated with Shanghai Huahuituo Pharmaceutical Technology Co., Ltd.

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Pipeline

Pipeline Snapshot as of 07 Nov 2024

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

Preclinical

IND Approval

Phase 1 Clinical

Current Projects

Drug(Targets)	Indications	Global Highest Phase

HHT120 ( thrombin )	Venous Thromboembolism More	Phase 1
HHT-109 ( JAK1 )	Rheumatoid Arthritis More	IND Approval
EZH2 Inhibitor(Synergy Pharmaceutical) ( EZH2 )	Lymphoma More	Preclinical
HHT-123 ( TYK2 )	Autoimmune Diseases More	Discovery
HHT-118 ( BTK )	Autoimmune Diseases More	Discovery

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