A Dose Regimen-Finding Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Activity of Oradoxel Monotherapy in Subjects With Advanced Malignancies

This is a nonrandomized, open-label, dose escalation, safety, activity, and PK study to determine the MTD and optimal dosing regimen of Oradoxel. No control group has been included.

Start Date20 Apr 2017

Sponsor / Collaborator

Athenex, Inc.

NCT04035473

/ CompletedPhase 1

A Randomized Crossover Study to Determine the Bioequivalence of Three Consecutive Daily Doses of Oraxol in Cancer Patients Treated With Intravenous Paclitaxel

This is a multicenter, open-label, 2-stage study with a 2-treatment period crossover design. Eligible participants are adults with cancer for whom weekly therapy with IV paclitaxel at a dose of 80 mg/m2 over 1 hour is indicated.
Stage 1 will consist of an initial cohort (Cohort 1) up to 6 evaluable participants who will receive a dosing regimen of Oraxol consisting of a 15-mg oral HM30181AK-US tablet plus an oral paclitaxel dose of 205 mg/m2, both administered once daily for 3 consecutive days. The stages and cohorts are further described in the "Study Design - Stages and Cohorts" table below. An interim analysis of pharmacokinetic (PK) data from Cohort 1 will be conducted to determine if the administered regimen would appear likely to achieve bioequivalence(BE) (AUC0-∞), if tested in a greater number of participants in Stage 2. If it appears unlikely that the selected regimen will meet the criteria for BE based on AUC0-∞ data, a second cohort (Cohort 2) of up to 6 evaluable participants may be enrolled in Stage 1, and the dose of paclitaxel in Oraxol may be adjusted by a maximum of +/- 25%. If Cohort 2 is enrolled, a second interim analysis will be conducted.
After the interim analysis/analyses (depending on the outcomes), a decision will be made by consensus of the Data Safety and Monitoring Board(DSMB), Kinex, Zenith Technology, and the Principal Investigator as to what dose should be administered in Stage 2. The DSMB will consist of a clinical oncologist, an ethicist, an independent statistician, and additional members, as deemed necessary. A DSMB charter will describe the planned evaluations and decision points used to determine the dose for Stage 2. An additional 18 to 42 evaluable participants will be enrolled into Stage 2 based on the Stage 1 results (AUC0-∞). Thus a total of up to 54 evaluable participants could potentially be enrolled in this study (6 each from Stage 1, Cohorts 1 and 2, and up to 42 participants in Stage 2).

Start Date01 Aug 2015

Sponsor / Collaborator

Athenex, Inc.

[+2]

100 Clinical Results associated with Encequidar mesylate

100 Translational Medicine associated with Encequidar mesylate

100 Patents (Medical) associated with Encequidar mesylate

Literatures (Medical) associated with Encequidar mesylate

01 Jun 2025·Veterinary and Comparative Oncology

Tolerability Assessment of Orally Administered Paclitaxel With Encequidar in Dogs With Spontaneous Malignancy

Article

Author: Press, Saya ; Ziegler, Jordan ; Istvan, Stephanie ; Cawley, Jacob ; Khanna, Chand ; Stewart, Samuel ; Fenger, Joelle

ABSTRACT:

Paclitaxel is an antimitotic agent that targets elements of the cancer phenotype, including cell proliferation, DNA repair, and apoptosis, predicting its broad activity in a spectrum of cancers. An oral paclitaxel formulation has been developed to overcome challenges associated with parenteral administration of this drug, notably the development of Cremophor‐induced acute hypersensitivity reactions, which are particularly problematic in dogs. The aim of this open‐label, dose‐escalating study was to evaluate the tolerability and determine the maximum tolerated dosage (MTD) and dose‐limiting toxicity (DLT) of oral paclitaxel when co‐administered with the P‐glycoprotein pump inhibitor, encequidar, in dogs with cancer. Paclitaxel was administered as a 3‐consecutive‐day course starting at 90 mg/m2 with encequidar weekly for 3 weeks, using escalation of 30 mg/m2 increments. MTD was established using a rolling‐six dose escalation study design, based on the number of dogs experiencing any DLT assessed after each dosing cycle and during a 28‐day post‐treatment monitoring period. Nineteen client‐owned dogs were enrolled. MTD was established at 90 mg/m2 and the most frequent adverse events (AEs) were gastrointestinal, followed by hematologic, with the majority being self‐resolving and low grade. VCOG Grades 3 and 4 gastrointestinal toxicity, Grade 4 neutropenia, and acute kidney injury were defined as DLTs at 120 mg/m2. Conclusions of this study define oral paclitaxel MTD in cancer‐bearing dogs at 90 mg/m2 when given with encequidar for 3 consecutive days weekly for 3 weeks. Future Phase 2 trials evaluating the therapeutic activity of oral paclitaxel at its MTD co‐administered with encequidar in defined tumour histologies are warranted.

01 Dec 2024·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel third generation P-glycoprotein inhibitors bearing an azo moiety with MDR-reversing effect

Article

Author: Wu, Yiqing ; Qiu, Jingying ; Zhao, Jiangyan ; Tan, Zhoupeng ; Niu, Mingshan ; Gu, Xiaoke ; Sun, Shuang ; Yuan, Weiqun ; Zeng, Meifeng ; Feng, Hao ; Li, Zheng

P-glycoprotein (P-gp)-caused multidrug resistance (MDR) is a crucial factor in the cancer chemotherapy failure. Herein, a total of twenty two azo-containing WK-X-34 (WK34, a third generation P-gp inhibitor) derivatives were synthesized as novel P-gp inhibitors. Biological evaluation revealed that compound 7i effectively reversed P-gp-mediated MDR in K562/A02 cells, with a higher reversal fold (RF) value than WK34 (142.79 vs. 64.41). Further investigation indicated that 7i dose-dependently inhibited P-gp function, without affecting its expression. CETSA results illustrated that 7i could obviously improve P-gp stability, suggesting its high affinity with P-gp. Molecular docking analysis revealed that 7i fit well into P-gp's binding pocket, thus displaying potent reversal effect on P-gp-mediated tumor MDR Optical properties evaluation confirmed that azo-containing 7i can undergo reversible changes in the cis and trans configurations under the irradiation of 365 nm and 520 nm wavelength of light. Notably, the configuration change of azo might affect the MDR-reversal potency, and cis-7i has a lower RF value than trans-7i (122.70 vs. 142.79), suggesting that development of photoswitchable P-gp inhibitors might be a novel strategy to reduce the systemic toxicity caused by indiscriminate inhibition of P-gp by traditional inhibitors. Collectively, 7i, as a novel P-gp inhibitor, warranted further investigation.

04 Nov 2024·ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Highly Potent and Intestine Specific P‐Glycoprotein Inhibitor to Enable Oral Delivery of Taxol

Article

Author: Liu, Lei ; Pan, Peichen ; Li, Lan ; Du, Juan ; Zhang, Xing ; Zhang, Ping ; Zhou, Xianjing ; Shi, Wei ; Lai, Zhencheng ; Cui, Sunliang ; Qian, Hai ; Yang, Yuyan

Abstract:

Taxol is widely used in cancer chemotherapy; however, the oral absorption of Taxol remains a formidable challenge. Since the intestinal p‐glycoprotein (P‐gp) mediated drug efflux is one of the primary causes, the development of P‐gp inhibitor is emerging as a promising strategy to realize Taxol's oral delivery. Because P‐gp exists in many tissues, the non‐selective P‐gp inhibitors would lead to toxicity. Correspondingly, a potent and intestine specific P‐gp inhibitor would be an ideal solution to boost the oral absorption of Taxol and avoid exogenous toxicity. Herein, we would like to report a highly potent and intestine specific P‐gp inhibitor to enable oral delivery of Taxol in high efficiency. Through a multicomponent reaction and post‐modification, various benzofuran‐fused‐piperidine derivatives were achieved and the biological evaluation identified 16 c with potent P‐gp inhibitory activity. Notably, 16 c was intestine specific and showed almost none absorption (F=0.82 %), but possessing higher efficacy than Encequidar to improve the oral absorption of Taxol. In MDA‐MB‐231 xenograft model, the oral administration of Taxol and 16 c showed high therapeutic efficiency and low toxicity, thus providing a valuable chemotherapy strategy.

News (Medical) associated with Encequidar mesylate

29 Sep 2025

·www.fiercebiotech.com

Gilead pumps up virology pipeline with drug transporter deal

Gilead Sciences\' deal with Health Hope Pharma opens another chapter in encequidar’s long development journey. \n Gilead Sciences has bolted another asset onto the virology engine that powers the company, paying (PDF) Health Hope Pharma $10 million upfront for global rights to a candidate in a limited set of indications.The deal will give Gilead exclusive global rights to the P-gp inhibitor encequidar in the virology space. In return, Gilead will pay HHP the upfront fee and commit up to $72.5 million in milestones. Hanmi Pharm, the original developer of the candidate, is also in line to receive an upfront fee and potential milestone payments tied to development, regulatory and sales events.HHP is studying encequidar in combination with oral paclitaxel in cancer patients, with a phase 3 trial set to start this year. In that context, encequidar’s selective inhibition of P-gp in the gut could counter the drug transporter effect that typically prevents oral dosing of chemotherapeutics such as paclitaxel.Gilead is yet to comment on how encequidar fits into its virology plans. Some antiviral drugs, including components of Gilead’s blockbuster Biktarvy, are substrates of P-gp. Giving such drugs at the same time as P-gp inhibitors can increase the absorption and plasma concentrations of the antiviral medicines. Interactions between P-gp inhibitors and antiviral drugs can be undesirable. The label of Gilead’s Yeztugo recommends (PDF) against giving the twice-yearly HIV prevention drug with P-gp inhibitors. Yet there is also potential for co-administration with P-gp inhibitors to enhance the efficacy of antivirals that target pathogens including HIV and hepatitis C. There is a long history of exploring P-gp inhibitors in such viral contexts. In 2001, a Roche scientist co-authored a paper about the potential for inhibitors of the drug transporter to improve HIV treatment by opening up pharmacological sanctuary sites such as the brain.Gilead’s deal opens another chapter in encequidar’s long development journey. Hanmi out-licensed the candidate to Athenex in 2011. Athenex took the candidate as far as a filing for approval, only for the FDA to raise concerns about the safety and efficacy of the company’s oral paclitaxel formulation. After Athenex filed for bankruptcy in 2023, HHP bought a portfolio of cancer programs from the company.

Phase 3Acquisition

29 Sep 2025

·www.prnewswire.com

Health Hope Pharma Enters into Exclusive Licensing Agreement with Gilead Sciences

HHP and Hanmi will grant Gilead exclusive license to encequidar, and provide access to drug supply HONG KONG, Sept. 29, 2025 /PRNewswire/ -- Health Hope Pharma Limited ("HHP") today announced that it has entered into a global licensing and collaboration agreement with Gilead Sciences, Inc. ("Gilead") for encequidar, a first-in-class P-glycoprotein ("P-gp") inhibitor in the field of virology. HHP is currently exploring the potential of using encequidar to develop oral drug formulations across multiple fields. The most advanced program of HHP is oral paclitaxel combined with encequidar in the field of oncology, targeting to replace intravenous paclitaxel in chemotherapy for metastatic breast cancer. HHP targets to recruit the first patients for its global phase III clinical study for sites in the U.S. and Hong Kong SAR, respectively, by the fourth quarter of 2025. Under the agreement, HHP and Hanmi Pharm ("Hanmi") will grant Gilead exclusive global rights to encequidar within the field of virology. In addition, HHP and Hanmi will provide drug supply, share technical know-how, and participate as key project partners. HHP and Hanmi will each receive an upfront payment and are eligible to receive development, regulatory and sales milestones in addition to low single-digit royalties on net sales. Prof . Dennis Lam, founder of HHP said: "We are pleased to announce the licensing agreement with Gilead and Hanmi. This demonstrates the potential of encequidar as a first-in-class P-gp inhibitor to create more oral formulations in multiple fields. This agreement is also a milestone of successful innovation for both the Hong Kong biotech industry and HHP as a biotech company headquartered in Hong Kong. We will build on this momentum to accelerate HHP's development of oral paclitaxel combined with encequidar and explore other applications of encequidar in oral formulations." Jae-Hyun Park, CEO of Hanmi said: "This agreement validates Hanmi's formulation technology and R&D capabilities, while also opening the door to new growth opportunities through collaboration with a leading global partner. We will continue to expand strategic partnerships that can accelerate innovation and patient access worldwide." HHP is preparing for the commencement of global clinical trials of oral paclitaxel combined with encequidar in the U.S., Hong Kong SAR, and New Zealand, with plans to launch the product in Europe, Asia, and the U.S. About Health Hope Pharma Health Hope Pharma is a clinical-stage oncology biopharma headquartered in HK SAR and with operations in the U.S. and the U.K., dedicated to developing novel oral anti-cancer drugs towards a safer and more convenient alternative to conventional intravenous therapy. Our flagship drug, oral paclitaxel combined with encequidar, aims to replace the widely used intravenous paclitaxel with its oral equivalent and improve the quality of life of patients. About Hanmi Pharm Hanmi Pharm is an R&D-focused pharmaceutical company committed to developing globally innovative therapies in areas of high unmet medical needs such as obesity/metabolism, oncology, and rare diseases. Hanmi leverages proprietary platform technologies, including long-acting biologics and bispecific antibodies, to address unmet medical needs. The company emphasizes open innovation and has established numerous global partnerships to advance its research and development efforts. Media Relations & Investor Relations [email protected] SOURCE Health Hope Pharma WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

License out/inPhase 3Drug Approval

29 Sep 2025

·www.prnewswire.com

Hanmi's Oral Delivery Platform Compound Licensed to Gilead

Hanmi and HHP will grant Gilead an exclusive license to Encequidar and provide access to drug supply. SEOUL, South Korea, Sept. 29, 2025 /PRNewswire/ -- Hanmi Pharm announced on September 29 that it has entered into a global licensing and collaboration agreement with Gilead Sciences, Inc. ("Gilead") and Health Hope Pharma ("HHP") granting Gilead the exclusive rights to develop and commercialize encequidar. Orascovery™ is an innovative oral drug delivery proprietary platform owned by Hanmi that enables the conversion of injectable medicines into oral formulations. Encequidar is a P-gp inhibitor that was discovered through Hanmi's Orascovery™ platform and originally developed by Hanmi. Under this agreement, Hanmi and HHP will grant Gilead exclusive global rights to Encequidar within the field of virology. Hanmi and HHP will also provide drug supply, share technical know-how, and participate as key project partners. Hanmi and HHP will each receive an upfront payment and remain eligible for development, regulatory and sales milestones in addition to low single digit royalties on net sales. Dr. Dennis Lam, founder of HHP said: "We are pleased to announce the licensing agreement with Gilead and Hanmi. This demonstrates the potential of Encequidar as a first-in-class P-gp inhibitor to create more oral formulations in multiple fields. This agreement is also a milestone of successful innovation for both the Hong Kong biotech industry and HHP as a biotech company headquartered in Hong Kong. We will build on this momentum to accelerate HHP's development of Oraxol and explore other applications of Encequidar in oral formulations." Jae-Hyun Park, CEO of Hanmi Pharm, said: "This agreement validates Hanmi's formulation technology and R&D capabilities, while also opening the door to new growth opportunities through collaboration with a leading global partner. We will continue to expand strategic partnerships that can accelerate innovation and patient access worldwide." Hanmi originally out-licensed Encequidar along with the oral anticancer drug Oraxol to Athenex in 2011. However, following Athenex's insolvency, rights were transferred to HHP and others. HHP is currently conducting clinical trials of Oraxol in the U.S., Hong Kong SAR, and New Zealand since June 2025, with plans to sequentially launch the product in Europe, Asia, and the U.S. Contact info: Official Websites: Official LinkedIn: [email protected], +08-2-410-0467 SOURCE Hanmi Pharm WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

License out/inDrug Approval

100 Deals associated with Encequidar mesylate

External Link

KEGG	Wiki	ATC	Drug Bank
D11783	-	-	DB14070

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Phase 1	China	Athenex, Inc.	15 Aug 2019
Breast Cancer	Phase 1	China	M.W. Encap Ltd.	15 Aug 2019
Solid tumor	Phase 1	United States	Athenex, Inc.	20 Apr 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis