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Overview

Tags

Neoplasms

Other Diseases

Skin and Musculoskeletal Diseases

Small molecule drug

Diagnostic radiopharmaceuticals

Therapeutic radiopharmaceuticals

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	9
Endocrinology and Metabolic Disease	5
Nervous System Diseases	4
Hemic and Lymphatic Diseases	2
Immune System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	8
Diagnostic radiopharmaceuticals	6
Therapeutic radiopharmaceuticals	3
Radiopharmaceuticals and diagnostic agent	2
Peptide Conjugate Radionuclide	2

Top 5 Target	Count

PSMA(Prostate-specific membrane antigen)	2
SSTR(Somatostatin receptor)	1
NET(Norepinephrine transporter)	1
SSTR2(Somatostatin receptor 2)	1

评价镓[68Ga]多特安肽注射液 PET/CT 对神经内分泌瘤（NETs）的诊断效能、药代动力学和安全性及比较镥[177Lu]氧奥曲肽注射液与长效奥曲肽在不可切除或转移性、进展性、分化良好（G1 和 G2）且生长抑素受体阳性的成人胃肠胰神经内分泌瘤患者中的安全性和有效性的诊疗一体化的Ⅲ期临床研究

[Translation] A phase III clinical study to evaluate the diagnostic efficacy, pharmacokinetics and safety of gallium [68Ga] dotetan injection PET/CT for neuroendocrine tumors (NETs) and to compare the safety and efficacy of lutetium [177Lu] oxyoctreotide injection with long-acting octreotide in adult patients with unresectable or metastatic, progressive, well-differentiated (G1 and G2) somatostatin receptor-positive gastrointestinal pancreatic neuroendocrine tumors

主要目的：基于相对于真实性标准的受试者水平的灵敏度和特异度，评价镓[68Ga]多特安肽注射液 PET/CT 对 NETs 的诊断效能。次要目的：评价镓[68Ga]多特安肽注射液作为 PET/CT 检查的示踪剂在中国人群中的安全性；评价镓[68Ga]多特安肽注射液作为 PET/CT 检查的示踪剂在中国人群中的药代动力学（PK）及辐射剂量学。

[Translation]

Primary objective: To evaluate the diagnostic efficacy of gallium [68Ga] dotetan injection PET/CT for NETs based on the sensitivity and specificity at the subject level relative to the authenticity standard. Secondary objectives: To evaluate the safety of gallium [68Ga] dotetan injection as a tracer for PET/CT examination in the Chinese population; To evaluate the pharmacokinetics (PK) and radiation dosimetry of gallium [68Ga] dotetan injection as a tracer for PET/CT examination in the Chinese population.

Start Date05 Jan 2024

Sponsor / Collaborator

HTA Co., Ltd.

CTR20234275

/ RecruitingPhase 3

评价锝[99mTc]硫化胶体注射液应用于乳腺癌患者前哨淋巴结示踪的有效性和安全性：一项自身对照临床研究

[Translation] Evaluation of the efficacy and safety of technetium [99mTc] sulfide colloid injection for sentinel lymph node tracing in breast cancer patients: a self-controlled clinical study

主要目的：评价锝[99mTc]硫化胶体注射液在乳腺癌患者中进行前哨淋巴结示踪的有效性；次要目的：评价锝[99mTc]硫化胶体注射液在乳腺癌患者中进行前哨淋巴结示踪的安全性；探索性目的：探索锝[99mTc]硫化胶体注射液注射前预处理时间对检出率的影响；探索手持伽马计数器对前哨淋巴结闪烁记数阳性阈值的合理性。

[Translation]

Primary purpose: To evaluate the effectiveness of technetium [99mTc] sulfide colloid injection in sentinel lymph node tracing in breast cancer patients; Secondary purpose: To evaluate the safety of technetium [99mTc] sulfide colloid injection in sentinel lymph node tracing in breast cancer patients; Exploratory purpose: To explore the effect of pretreatment time before technetium [99mTc] sulfide colloid injection on the detection rate; To explore the rationality of the positive threshold of sentinel lymph node scintigraphy by handheld gamma counter.

Start Date02 Jan 2024

Sponsor / Collaborator

HTA Co., Ltd.

100 Clinical Results associated with HTA Co., Ltd.

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0 Patents (Medical) associated with HTA Co., Ltd.

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52

Literatures (Medical) associated with HTA Co., Ltd.

01 Feb 2025·Current Organic Chemistry

Bispidine-based Ligands as Bifunctional Chelators for Radiopharmaceuticals

Author: Li, Rui ; Yan, Yuting ; Huang, Jianhui ; Ren, Xiyan ; Li, Hongyu

Novel bispidine skeleton has been extensively designed as bifunctional chelators (BFCs) for their special stereochemical structure and variable dentate numbers. Bispidinebased ligands (BBLs) as BFCs generally integrate the benefits of conventional acyclic and macrocyclic BFCs, demonstrating exceptional radiolabeling kinetics, thermodynamic stability and kinetic inertness for their metal complexes. The accessible inherent spatial asymmetry in bispidine skeleton is well-suited for Jahn-Teller active metal ions, notably Cu(II). Currently, BBLs have already been studied to coordinate with radionuclides such as 52Mn, 64/67Cu, 68Ga, 111In, 133La, 177Lu, 212Pb, 212/213Bi, and 225Ac for radiopharmaceuticals application. Among them, the 64Cu, 52Mn, 111In, 177Lu, and 225Ac complexes with BBLs have particularly made significant research progress. In this review, we introduce the synthesis of BBLs and their applications in chelating the above five metallic radionuclides for the development of radiopharmaceuticals are discussed.

01 Nov 2024·European Journal of Pharmacology

Dual inhibition of topoisomerase II and microtubule of podophyllotoxin derivative 5p overcomes cancer multidrug resistance

Article

Author: Li, Xiao-xue ; Gong, Jian-hua ; Dong, Yan-Qun ; Zou, Zhong-mei ; Hong, Han-yu ; Zou, Zhong-Mei ; Dong, Yan-qun ; Zheng, Yan-bo ; Zheng, Yi-Jia ; Li, Xiao-Xue ; Cheng, Wei-hua ; Hong, Han-Yu ; Shang, Hai ; Zheng, Yan-Bo ; Zheng, Yi-jia ; Cheng, Wei-Hua ; Zhang, Jun-Yi ; Lv, Xing ; Zhang, Jun-yi ; Gong, Jian-Hua

Compound 5p is a 4β-N-substituted podophyllotoxin derivative, which exhibited potent activity toward drug-resistant K562/A02 cells and decreased MDR-1 mRNA expression. Here, we further investigated its detail mechanism and tested its antitumor activity. 5p exerted catalytic inhibition of topoisomerase IIα, and didn't show the inhibitor of topoisomerase I. 5p exhibited the inhibitory effect on microtubule polymerization. 5p showed potent anti-proliferation against breast cancer, oral squamous carcinoma, and their drug-resistant cell lines, with resistance index of 0.61 and 0.86, respectively. 5p downregulated the expression levels of P-gp in KB_V200 cells and BCRP in MCF7/ADR cells in dose-dependent manner. Moreover, 5p induced KB and KB_V200 cells arrest at G₂/M phase by up-regulating the expression of γ-H2AX, p-Histone H3 and cyclin B1. 5p induced apoptosis and pyroptosis by increased the expression levels of cleaved-PARP, cleaved-caspase3, N-GSDME as well as LDH release in KB and KB_V200 cells. In addition, 5p efficiently impaired tumor growth in KB and KB_V200 xenograft mice. Conclusively, this work elucidated the dual inhibitor of topoisomerase II and microtubule of 5p and its mechanism of overcoming the multidrug resistance, indicating that 5p exerts the antitumor potentiality.

05 Aug 2024·Molecular Pharmaceutics

Preparation of Radiolabeled Zolbetuximab Targeting CLDN18.2 and Its Preliminary Evaluation for Potential Clinical Applications

Article

Author: Ma, Lin ; Li, Dengke ; Kuang, Zijun ; Yang, Jian ; Wang, Yang ; Li, Zheng ; Liu, Yuxia ; Zhang, Lan ; Li, Qingnuan

Claudin18.2 (CLDN18.2), due to its high expression in various gastric cancer tissues, is considered an optimal target for antitumor drug molecules. In this study, we obtained the labeled compounds of [¹²⁵I]I-zolbetuximab using the Iodogen method. Under the optimum labeling conditions, the molar activity of [¹²⁵I]I-zolbetuximab was 1.75 × 10² GBq/μmol, and the labeling efficiency was more than 99%. The labeled compounds exhibited excellent in vitro stability in both phosphate buffer saline (PBS, pH = 7.4) and fetal bovine serum systems (FBS) (radiochemical purity >90% at 72 h). The uptake percentage of [¹²⁵I]I-zolbetuximab in MKN45-CLDN18.2 cells is 24.69 ± 0.84% after 6 h. The saturation binding assay and specificity assay further demonstrated the high specificity of [¹²⁵I]I-zolbetuximab for CLDN18.2. The long retention at the tumor site and rapid metabolic clearance at other organ sites of [¹²⁵I]I-zolbetuximab were observed in small-animal SPECT-CT imaging. The same trend was also observed in the biodistribution study. Due to the excellent targeting ability of zolbetuximab for CLDN18.2, [¹²⁵I]I-zolbetuximab exhibits strong specific binding and retention with cells and tumors highly expressing CLDN18.2. However, the balance between mAb's longer cycle time in vivo and targeting binding and retention ability should be intensively considered for using this kind of radiopharmaceutical in the diagnosis and treatment of CLDN18.2-positive gastric cancer.

100 Deals associated with HTA Co., Ltd.

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100 Translational Medicine associated with HTA Co., Ltd.

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Pipeline

Pipeline Snapshot as of 30 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

1

Preclinical

Phase 1 Clinical

1

Phase 2 Clinical

Phase 3 Clinical

6

3

Approved

Other

3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Technetium Tc-99M Sestamibi Kit	Heart Diseases More	Approved
Methoxy Isobutyl Isonitrile	-	Approved
Fludeoxyglucose F-18	Neoplasms More	Approved
Iobenguane I-131 ( NET )	Pheochromocytoma More	Phase 3
Technetium Tc-99M Sulfur Colloid	Invasive Mammary Carcinoma More	Phase 3