Delving into the Latest Updates on Orbitazine fumarate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Orbit azine fumarate, 富马酸奥比特嗪肠溶微丸胶囊

Target

caspase 3

Action

activators

Mechanism

caspase 3 activators(Caspase-3 activators)

Therapeutic Areas

NeoplasmsNervous System DiseasesDigestive System Disorders+ [2]

Active Indication

High grade gliomaAdvanced Triple-Negative Breast CarcinomaAdenocarcinoma of small intestine+ [6]

Inactive Indication

Advanced Malignant Solid NeoplasmRecurrent LymphomaRefractory Lymphoma

Originator Organization

Shenzhen Zhenxing Pharmaceutical Technology Co Ltd

Active Organization

Shenzhen Zhenxing Pharmaceutical Technology Co Ltd

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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1、主要目的：评价富马酸奥比特嗪肠溶微丸胶囊（SM-1）治疗晚期小肠腺癌的有效性。 2、次要目的：（1）评价富马酸奥比特嗪肠溶微丸胶囊（SM-1）治疗晚期小肠腺癌的安全性；（2）评价富马酸奥比特嗪肠溶微丸胶囊（SM-1）治疗晚期小肠腺癌的PK、PD特征。

[Translation]

1. Primary objective: To evaluate the efficacy of Orbitazine fumarate enteric-coated micropellets (SM-1) in the treatment of advanced small intestinal adenocarcinoma. 2. Secondary objectives: (1) To evaluate the safety of Orbitazine fumarate enteric-coated micropellets (SM-1) in the treatment of advanced small intestinal adenocarcinoma; (2) To evaluate the PK and PD characteristics of Orbitazine fumarate enteric-coated micropellets (SM-1) in the treatment of advanced small intestinal adenocarcinoma.

Start Date03 Jan 2023

Sponsor / Collaborator

Shenzhen Zhenxing Pharmaceutical Technology Co Ltd

CTR20221641

/ Active, not recruitingPhase 1

富马酸奥比特嗪肠溶微丸胶囊（SM-1）联合替莫唑胺在难治或复发胶质母细胞瘤受试者中的安全性、药代动力学 I 期临床研究

[Translation] Phase I clinical study on the safety and pharmacokinetics of orbitazine fumarate enteric-coated micropellets (SM-1) combined with temozolomide in subjects with refractory or recurrent glioblastoma

主要目的：确定富马酸奥比特嗪肠溶微丸胶囊（SM-1）联合替莫唑胺在复发高级别胶质瘤患者的安全性和耐受性，包括剂量限制性毒性（DLT）和最大耐受剂量（MTD）/II 期推荐剂量（RP2D）。次要目的： 1）确定富马酸奥比特嗪肠溶微丸胶囊（SM-1）联合替莫唑胺在复发高级别胶质瘤患者中口服给药的药代动力学特性； 2）初步评估富马酸奥比特嗪肠溶微丸胶囊（SM-1）在中国复发高级别胶质瘤患者中的有效性。

[Translation]

Primary objective: To determine the safety and tolerability of oral SM-1 combined with temozolomide in patients with recurrent high-grade glioma, including dose-limiting toxicity (DLT) and maximum tolerated dose (MTD)/phase II recommended dose (RP2D). Secondary objectives: 1) To determine the pharmacokinetic properties of oral SM-1 combined with temozolomide in patients with recurrent high-grade glioma; 2) To preliminarily evaluate the efficacy of SM-1 in Chinese patients with recurrent high-grade glioma.

Start Date19 Sep 2022

Sponsor / Collaborator

Shenzhen Zhenxing Pharmaceutical Technology Co Ltd

CTR20200351

/ CompletedPhase 1

富马酸奥比特嗪肠溶微丸胶囊（SM-1）在晚期实体瘤及复发难治性淋巴瘤患者的安全性、药代动力学I期临床研究

[Translation] Phase I clinical study on the safety and pharmacokinetics of Orbitazine Fumarate Enteric-coated Micropellets (SM-1) in patients with advanced solid tumors and relapsed and refractory lymphoma

1.主要目的确定富马酸奥比特嗪肠溶微丸胶囊（SM-1）在晚期实体瘤及复发难治性淋巴瘤患者的安全性和耐受性，包括剂量限制性毒性（DLT）和最大耐受剂量（MTD）/II 期推荐剂量（RP2D）。 2. 次要目的确定富马酸奥比特嗪肠溶微丸胶囊（SM-1）单次、多次口服给药的药代动力学特征。初步评估富马酸奥比特嗪肠溶微丸胶囊（SM-1）的抗肿瘤活性。

[Translation]

1. Primary Objective To determine the safety and tolerability of Orbitazine Fumarate Enteric-Coated Micropellets Capsules (SM-1) in patients with advanced solid tumors and relapsed refractory lymphoma, including dose-limiting toxicity (DLT) and maximum tolerated dose (MTD)/Phase II recommended dose (RP2D). 2. Secondary Objective To determine the pharmacokinetic characteristics of Orbitazine Fumarate Enteric-Coated Micropellets Capsules (SM-1) after single and multiple oral administration. To preliminarily evaluate the antitumor activity of Orbitazine Fumarate Enteric-Coated Micropellets Capsules (SM-1).

Start Date27 Apr 2020

Sponsor / Collaborator

Shenzhen Zhenxing Pharmaceutical Technology Co Ltd

100 Clinical Results associated with Orbitazine fumarate

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100 Translational Medicine associated with Orbitazine fumarate

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100 Patents (Medical) associated with Orbitazine fumarate

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1

Literatures (Medical) associated with Orbitazine fumarate

01 Sep 2020·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

In vitro metabolic characterization of orbitazine, a novel derivative of the PAC-1 anticancer agent

Q3 · MEDICINE

Article

Author: Zhu, Qubo ; Han, Xuhua ; Wang, Shanshan ; Chen, Yanfen ; Hu, Gaoyun ; Liu, Wenjie ; Cheng, Zeneng ; Li, Fang

AbstractObjectivesThe in vitro evaluation of new drugs is an important step in the drug development pipeline. Orbitazine is a derivative of PAC-1 that has substituted the functional group homopiperazine ring with a piperazine ring. The purpose of this study was to assess the metabolic profile of orbitazine.MethodsMetabolism was characterized in vitro by incubating liver microsomes with metabolize orbitazine or the classical metabolic enzyme substrates. High performance liquid chromatography (HPLC) and LC-MS/MS were used to identify the parent drugs and metabolites of orbitazine or metabolic enzyme substrates.Key findingsThere was no difference in metabolic stability or metabolites across different species. The metabolites included a debenzyl compound and several hydroxyl compounds, defined as M1(316), M2(440), M3(422), M4(422) and M5(422). We found that orbitazine was metabolized by CYP3A4, CYP2C9 and CYP2D6 in a human liver microsomes incubation system. Orbitazine had no significant inhibitory effect on CYP1A2, CYP2B6, CYP2C9, or CYP2C19 in human liver microsomes, but showed a dose-dependent inhibition of CYP2C8, CYP2D6 and CYP3A4; and there was no orbitazine-mediated induction of CYP1A2, CYP2B6, CYP3A4 or mRNA expression in hepatocytes.ConclusionsThis in vitro data on the metabolism of orbitazine may provide valuable information to support further clinical progression as a potential therapeutic molecule.

100 Deals associated with Orbitazine fumarate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 3	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	27 Apr 2020
Recurrent Lymphoma	Phase 3	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	27 Apr 2020
Refractory Lymphoma	Phase 3	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	27 Apr 2020
High grade glioma	Phase 2	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	23 Aug 2024
Advanced Triple-Negative Breast Carcinoma	Phase 2	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	21 Apr 2023
Adenocarcinoma of small intestine	Phase 2	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	03 Jan 2023
Colonic Cancer	Phase 2	-	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	-
Glioma	Phase 2	-	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	-
Rectal Cancer	Phase 2	-	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	-
Head and Neck Neoplasms	Phase 1	China	Shenzhen Zhenxing Pharmaceutical Technology Co Ltd	-