Delving into the Latest Updates on Encequidar mesylate/Irinotecan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Encequidar/irinotecan, Irinotecan/HM 30181A, Irinotecan/HM30181AK

+ [3]

Target

P-gp x Top I

Action

inhibitors

Mechanism

P-gp inhibitors(P-glycoprotein 1 inhibitors), TOP1 inhibitors(DNA topoisomerase I inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication

Breast Cancer

Inactive Indication

Advanced cancerAdvanced Malignant Solid NeoplasmColorectal Cancer

Originator Organization

Hanmi Pharmaceutical Co., Ltd.

Active Organization

Athenex, Inc.

Inactive Organization

Hanmi Pharmaceutical Co., Ltd.

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC33H45ClN4O9

InChIKeyKLEAIHJJLUAXIQ-JDRGBKBRSA-N

CAS Registry136572-09-3

View All Structures (2)

主要目的：向在研究 KX-ORAX-CN-007中完成了Oraxol治疗，获得完全缓解（CR），部分缓解（PR），或病情稳定（SD），且希望继续治疗的患者和其他转移性乳腺癌患者提供进一步治疗，并进一步评估Oraxol在乳腺癌患者中的安全性。次要目的：进一步评估Oraxol 在乳腺癌患者中的有效性

[Translation]

Primary objective: To provide further treatment to patients who have completed Oraxol treatment in study KX-ORAX-CN-007 and achieved complete remission (CR), partial remission (PR), or stable disease (SD) and wish to continue treatment, and to other patients with metastatic breast cancer, and to further evaluate the safety of Oraxol in patients with breast cancer. Secondary objective: To further evaluate the effectiveness of Oraxol in patients with breast cancer

Start Date29 Aug 2019

Sponsor / Collaborator

Athenex, Inc.

[+3]

CTR20191661

/ Active, not recruitingPhase 1

一项给予转移性乳腺癌患者Oraxol的延伸研究

[Translation] An extension study of Oraxol in patients with metastatic breast cancer

主要目的：向在研究 KX-ORAX-CN-007中完成了Oraxol治疗，获得完全缓解（CR），部分缓解（PR），或病情稳定（SD），且希望继续治疗的患者和其他转移性乳腺癌患者提供进一步治疗，并进一步评估Oraxol在乳腺癌患者中的安全性。次要目的：进一步评估Oraxol 在乳腺癌患者中的有效性

[Translation]

Primary objective: To provide further treatment to patients who have completed Oraxol treatment in study KX-ORAX-CN-007 and achieved complete remission (CR), partial remission (PR), or stable disease (SD) and wish to continue treatment, and to other patients with metastatic breast cancer, and to further evaluate the safety of Oraxol in patients with breast cancer. Secondary objective: To further evaluate the effectiveness of Oraxol in patients with breast cancer

Start Date29 Aug 2019

Sponsor / Collaborator

Athenex, Inc.

[+3]

CTR20190553

/ Active, not recruitingPhase 1

一项确定Oraxol在乳腺癌患者中药代动力学的临床研究

[Translation] A clinical study to determine the pharmacokinetics of Oraxol in breast cancer patients

主要目的：考察乳腺癌患者口服HM30181A和紫杉醇（Oraxol）的PK（AUC）次要目的：确定Oraxol在乳腺癌患者中的安全性和有效性（疗效率，无进展生存[PFS]），总生存[OS]）

[Translation]

Primary objective: To investigate the PK (AUC) of oral HM30181A and paclitaxel (Oraxol) in patients with breast cancer Secondary objective: To determine the safety and efficacy (efficacy rate, progression-free survival [PFS], overall survival [OS]) of Oraxol in patients with breast cancer

Start Date29 Apr 2019

Sponsor / Collaborator

Athenex, Inc.

[+3]

100 Clinical Results associated with Encequidar mesylate/Irinotecan

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100 Translational Medicine associated with Encequidar mesylate/Irinotecan

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100 Patents (Medical) associated with Encequidar mesylate/Irinotecan

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1

Literatures (Medical) associated with Encequidar mesylate/Irinotecan

01 Aug 2022·Cancer Chemotherapy and Pharmacology

A dose regimen-finding study to evaluate the safety, tolerability, pharmacokinetics, and activity of oratecan in subjects with advanced malignancies

Article

Author: Wang, Hui ; Zhi, Jay ; Chan, Wing-Kai ; Corr, Bradley ; Boland, Patrick M ; Ma, Wen Wee ; Redman, Michelle ; Jimeno, Antonio ; Fountzilas, Christos ; Diamond, Jennifer R ; Cutler, David ; Fakih, Marwan ; Opyrchal, Mateusz ; Kwan, Rudolf ; Kramer, Doug

PURPOSEIrinotecan is a commonly used chemotherapeutic in solid tumor malignancies. Oratecan is an investigational product comprised of encequidar methanesulfonate, a novel minimally absorbed P-glycoprotein pump inhibitor, and irinotecan. This study sought to determine the maximum tolerated dose (MTD) of oratecan in patients with advanced malignancies.METHODSUsing a "3 + 3″ dose-escalation design, patients were treated with oratecan on day 1 every 21 days. The irinotecan dose was escalated from 20 to 320 mg/m². The encequidar methanesulfonate dose was fixed at 15 mg (12.9 mg free base). PK sampling for irinotecan, encequidar and its major metabolites was performed following a single dose of oratecan during cycle 1. Patients were treated until disease progression or unacceptable toxicity.RESULTSThirty-five patients were treated. The MTD was determined to be 280 mg/m² every 21 days. Irinotecan and SN-38 plasma concentration-time profile showed that irinotecan exposure increased with dose and followed biexponential decay. Nine of 17 patients at oratecan dose levels 200 mg/m² and above had SN-38 exposures comparable to those with intravenous irinotecan at standard dosing. None of the 35 patients achieved a radiologic response, ten patients had SD for > 8 weeks; the median progression-free survival for all treated patients was 9 weeks (95% CI 8.6-13.9).CONCLUSIONSThe MTD of oratecan was encequidar methanesulfonate 15 mg plus irinotecan 280 mg/m². Exposure for irinotecan and SN-38 increased with increased dose. Potential antitumor activity was observed at the 280 and 320 mg/m² dose levels. The safety profile of oratecan was comparable to that of intravenous irinotecan.

100 Deals associated with Encequidar mesylate/Irinotecan

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colorectal Cancer	Phase 3	South Korea	Hanmi Pharmaceutical Co., Ltd.	18 May 2020
Solid tumor	Phase 3	United States	Athenex, Inc.	05 Sep 2014
Advanced cancer	Phase 3	South Korea	Hanmi Pharmaceutical Co., Ltd.	01 Dec 2010
Advanced Malignant Solid Neoplasm	Phase 3	South Korea	Hanmi Pharmaceutical Co., Ltd.	01 Jun 2008
Breast Cancer	Phase 1	China	Athenex, Inc.	29 Apr 2019

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01463982 (CTgov)	Phase 1	Advanced Malignant Solid Neoplasm \| Advanced cancer	21	Oratecan+Capecitabine (Capecitabine 800mg/㎡ + Oratecan 10mg/㎡)	gdmyrtwfjw(ewmwqnupjl) = dijcufxufh uinupjtdrd (dsvsvidpsk, oshdmnzbex - kwbjhnmvpg) View more	-	23 Apr 2015
				Oratecan+Capecitabine (Capecitabine 800mg/㎡ + Oratecan 15mg/㎡)	gdmyrtwfjw(ewmwqnupjl) = ozmfiqgfdw uinupjtdrd (dsvsvidpsk, exsarsbmfd - zvoyvfawnn) View more