[Translation] Pharmacokinetics and safety of HC-1119 softgels in male subjects with mild hepatic impairment (Child-Pugh: Class A), moderate hepatic impairment (Child-Pugh: Class B), and normal hepatic function Phase I clinical study of

主要目的评估HC-1119软胶囊在轻度肝功能不全（Child-Pugh：A级）、中度肝功能不全（Child-Pugh：B级）和肝功能正常的男性受试者中的药代动力学（PK）特征，为HC-1119软胶囊的临床应用提供依据。次要目的评估HC-1119软胶囊在轻度肝功能不全（Child-Pugh：A级）、中度肝功能不全（Child-Pugh：B级）和肝功能正常的男性受试者中的安全性。

[Translation]

main purpose To assess the pharmacokinetics (PK ) characteristics, which provide a basis for the clinical application of HC-1119 soft capsules. secondary purpose To evaluate the safety of HC-1119 soft capsules in male subjects with mild hepatic insufficiency (Child-Pugh: class A), moderate hepatic insufficiency (Child-Pugh: class B), and normal hepatic function.

Start Date26 Nov 2021

Sponsor / Collaborator

Hinova Pharmaceuticals, Inc.

CTR20212160 / CompletedPhase 1

[14C] HC-1119在中国成年男性健康受试者体内的吸收、代谢和排泄临床试验-[14C] HC-1119的人体物质平衡及生物转化研究

[Translation] [14C] HC-1119 Absorption, Metabolism and Excretion Clinical Trial of Chinese Adult Male Healthy Subjects-Human Mass Balance and Biotransformation of [14C] HC-1119

主要目的 1、定量分析男性健康受试者口服[14C] HC-1119后排泄物中的总放射性，获得人体放射性回收率数据和主要排泄途径； 2、鉴定男性健康受试者口服[14C] HC-1119后人体内的主要代谢产物，确定主要生物转化途径和主要代谢产物（接近或>10%总放射性AUC）； 3、考察中国成年男性健康受试者单次口服[14C] HC-1119后全血和血浆中的分配情况和血浆中总放射性的药代动力学； 4、采用已验证的液相色谱串联质谱联用法（LC-MS/MS）定量分析血浆中 HC-1119和主要代谢产物（M1和M2），获得相应药代动力学参数；次要目的 1、评价[14C]HC-1119单次给药后健康受试者的安全性。

[Translation]

main purpose 1. Quantitatively analyze the total radioactivity in the excreta of male healthy subjects after oral administration of [14C]HC-1119, and obtain the data on the recovery rate of radioactivity in humans and the main excretion route; 2. Identify the main metabolites in the human body after oral administration of [14C]HC-1119 in male healthy subjects, and determine the main biotransformation pathways and main metabolites (close to or >10% total radioactive AUC); 3. Investigate Chinese adult male health Distribution in whole blood and plasma and pharmacokinetics of total radioactivity in plasma after a single oral dose of [14C]HC-1119 in subjects; 4. Quantitative analysis of HC-1119 and major metabolites (M1 and M2) in plasma by a validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method to obtain the corresponding pharmacokinetic parameters; secondary purpose 1. To evaluate the safety of [14C]HC-1119 in healthy subjects after a single dose.

Start Date08 Nov 2021

Sponsor / Collaborator

Hinova Pharmaceuticals, Inc.

100 Clinical Results associated with Deuterated enzalutamide

100 Translational Medicine associated with Deuterated enzalutamide

100 Patents (Medical) associated with Deuterated enzalutamide

Literatures (Medical) associated with Deuterated enzalutamide

01 Nov 2023·Current Medicinal Chemistry

Clinical Application and Synthesis Methods of Deuterated Drugs

Article

Author: Rao, Guo-Wu ; Zhang, Wen ; Xu, Xiao-Liang

Abstract:Many drugs have adverse absorption, distribution, metabolism, and excretory (ADME) properties that prevent their widespread use or limit their use in some indications. In addition to preparation techniques and prodrug strategies, deuterium modification is a viable method for improving ADME properties. Deuterated drugs have attracted increasing attention from the pharmaceutical industry in recent years. To date, two deuterated drugs have been approved by the FDA. In 2017, austedo was approved by the FDA as a new drug for Huntington's disease in the United States, the first deuterium drug to be marketed worldwide. Recently (June 9, 2021), donafinil has been listed in China; this result has caused major pharmaceutical companies and the pharmaceutical industry to pay attention to deuterium technology again. In addition, BMS-986165, RT001, ALK-001, HC-1119, AVP-786 and other drugs are in phase III clinical studies, and some solid deuterium compounds have entered phase I and II clinical trials. The deuterium strategy has been widely used in pharmaceutical research and has become a hot spot in pharmaceutical research in recent years. In this paper, the research and development of deuterated drugs are reviewed, and the influence of deuterium modification on drugs, the advantages of deuterium strategies and the synthesis strategies of deuterated drugs are mainly introduced. Hoping to provide references for clinical application, the discovery of new deuterium chemical entities and research and development of new deuterated drugs.

01 Oct 2022·Molecular Biology Reports

HC-1119, a deuterated Enzalutamide, inhibits Migration, Invasion and Metastasis of the AR-positive triple-negative breast Cancer cells

Article

Author: Yang, Mao ; Liu, Xunxi ; Li, Xinghai ; Gao, Mengdi ; He, Tao ; Wu, Xuehong ; Gan, Lin ; Feng, Wanru

AbstractTriple-negative breast cancers (TNBCs) are aggressive, and they develop metastasis at earlier stages, relapse more frequently, and exhibits poorer prognosis than other subtypes of breast cancer. Due to the lack of estrogen receptor for endocrine therapy and HER2 for targeted therapy, new targeted therapies for TNBCs are urgently needed. Enzalutamide is a second-generation androgen receptor (AR) inhibitor, and HC-1119 is a new synthetic deuterated enzalutamide. Owing to the isotope effect, HC-1119 has many advantages over enzalutamide, including slow metabolism, high plasma concentration and low brain exposure. However, the efficacy of HC-1119 in inhibition of AR function in triple-negative breast cancer (TNBC) has not been studied. In this study, we found high-level AR expression in both Hs578T and SUM159PT TNBC cell lines. Activation of AR by dihydrotestosterone (DHT) in both cell lines increased AR protein, induced AR-nuclear localization, enhanced cell migration and invasion in culture, and promoted liver metastasis in mice. Importantly, cotreatment with HC-1119 of these cells efficiently abolished all of these effects of DHT on both Hs578T and SUM159PT cells. These results indicate that HC-1119 is a very effective new second-generation AR antagonist that can inhibit the migration, invasion and metastasis of the AR-positive TNBC cells.

01 Feb 2022·The ProstateQ3 · MEDICINE

Phase I clinical trial of HC‐1119 soft capsule in Chinese healthy adult male subjects: Pharmacokinetics and safety of single‐dose proportionality and effects of food

Q3 · MEDICINE

Article

Author: Gao, Shen ; Ni, Jin ; Zhou, Tie ; Cai, Tingting ; Li, Song ; Kang, Xin ; Tang, Shouyan ; Ma, Haiping ; Zhao, Naping ; Xu, Weidong ; Xiu, Jianping ; Zhang, Li

AbstractBackgroundPreclinical studies showed that HC‐1119, a deuterated version of enzalutamide, could competitively inhibit androgen binding to androgen receptor by blocking the transmission of androgen receptor signaling pathway as enzalutamide, inducing apoptosis of prostate cancer cells and reducing the proliferation of prostate cancer cells. Animal pharmacokinetic studies also show that deuterization of enzalutamide as HC‐1119 could retain the basic properties of mother drug, increases the stability of compounds to metabolic enzymes and the drug exposure in vivo, prolong the half‐life and reduce the production of metabolites, which may lead to a better efficacy and safety of HC‐1119 compared with enzalutamide.MethodsTo evaluate the pharmacokinetics and safety of HC‐1119 and the effects of food on pharmacokinetics in healthy adult Chinese men after single‐dose administration of HC‐1119. A total of 47 Chinese healthy adult male subjects received HC‐1119 soft capsule at a single oral dose of 40, 80, or 160 mg followed on fasting or 160 mg after high‐fat meal respectively. HC‐1119 prototype and its metabolites M1 and M2 in plasma were collected individually in a total 23 time points. Pharmacokinetics were determined by sensitive LC/MS/MS for dose‐proportionality study.ResultsIn subjects taking HC‐1119 soft capsules on fasting, Cmax of HC‐1119 prototype increased dose‐dependently. Either Cmax and AUC0‐∞ of M1 or Cmax of M2 showed statistically significant difference. Dose‐proportionality evaluation showed linear pharmacokinetic characteristics in Cmax of HC‐1119 prototype, Cmax and AUC0‐∞ of M2 in dose range of 40–160 mg. Cmax of HC‐1119 was significantly different between the two groups as 160 mg HC‐1119 on fasting or after a high‐fat diet respectively, while the other parameter were not. HC‐1119 and its metabolites M1 and M2 showed a linear dynamic trend.ConclusionsHC‐1119 is expected to have lower clinical dose than the similar drug enzalutamide. The absorption of HC‐1119 and the main pharmacokinetic parameters of HC‐1119 and its metabolites M1 and M2 were not affected by high‐fat diet. The clinical application of HC‐1119 soft capsule in the later stage can be recommended for both fasting and postprandial. The safety and tolerance were good in this population.

News (Medical) associated with Deuterated enzalutamide

13 Dec 2023

·www.prnewswire.com

Metastatic Prostate Cancer Market to Exhibit Positive Growth at a CAGR of 22% and 7.5% for mHSPC and mCRPC, respectively During the Study Period (2019-2032), Assesses DelveInsight

The dynamics of the metastatic prostate cancer market are anticipated to change in the coming years owing to the rise in the number of companies taking interest in the development of specific drugs for mCRPC and nmCRPC along with increasing awareness and penetration of already approved prostate cancer drugs. LAS VEGAS, Dec. 13, 2023 /PRNewswire/ -- DelveInsight's Metastatic Prostate Cancer Market Insights report includes a comprehensive understanding of current treatment practices, metastatic prostate cancer emerging drugs, market share of individual therapies, and current and forecasted market size from 2019 to 2032, segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain) and the United Kingdom, and Japan]. Key Takeaways from the Metastatic Prostate Cancer Market Report As per DelveInsight analysis, the total market size in the 7MM for metastatic castration-resistant prostate cancer (mCRPC) was estimated to be nearly USD 6.4 billion in 2022, which is expected to show positive growth by 2032. In 2022, the United States held the highest market share for mCRPC and mCSPC in the 7MM, at 63% and 61%, respectively, followed by the EU4 countries and the UK. As per DelveInsight estimates, the total prevalent population of prostate cancer in the 7MM was nearly 8 million cases in 2022. These cases will increase during the study period, i.e., 2019–2032. Leading metastatic prostate cancer companies such as AstraZeneca, Merck Sharp & Dohme, Hinova Pharmaceuticals, Pfizer, Astellas Pharma, Modra Pharmaceuticals, AB Science, Eli Lilly and Company, Zr Pharma & GmbH, Bristol-Myers Squibb, Ipsen, Exelixis, Takeda, Janssen Research & Development, Tesaro, Lantheus Holdings, Kintor Pharmaceutical, MacroGenics, Daiichi Sankyo, Madison Vaccines, Novartis, Point Biopharma, Xencor, Essa Pharma , Telix International, Bayer, Arvinas, and others are developing novel metastatic prostate cancer drugs that can be available in the metastatic prostate cancer market in the coming years. The promising metastatic prostate cancer therapies in the pipeline include HC-1119, Talazoparib, Enzalutamide, Niraparib, Boosted Oral Docetaxel, Masitinib, EPI-7386, Verzenio, 177Lu-PSMA-617, Capivasertib, I-131-1095, Proxalutamide (GT0918), MGC018, DS-7300, MVI-816, ARV-110, 177Lu-PNT2002 (PNT2002), Vudalimab (XmAb20717), 177Lu-DOTA-rosopatamab (TLX591), and others. Established therapies in the metastatic prostate cancer market include Astella/Pfizer's and Jansenn's blockbuster products XTANDI and ZYTIGA, respectively, approved for metastatic patients for over a decade now. Even though ZYTIGA's generics have entered the US market since 2019, and the EU since late 2022, leading to a drastic decline in the revenue mainly in the US, the product is extensively being evaluated in combination with novel emerging therapies, leading to an increase in patient share on the compound abiraterone acetate. Whereas, Jansenn's XTANDI, the biggest revenue generator in the prostate cancer market, has witnessed stable growth since 2021 owing to increased competition. Quantitatively mCRPC pipeline seems to be quite strong, however with recent failures/terminations of several trials of certain therapies in the past year, we have mentioned the most promising ones, which include ESSA Pharma's EPI-7386, Macrogenics, and Daiichi's anti-B7-H3 Antibody Drug Conjugates, MGC-018 and DS-7300 respectively, Arvinas, AR-targeted PROTAC protein degrader, and Point Biopharma's Radioligand therapy. Except for Point Biopharma's therapy, none of these potential players have initiated a Phase III trial, even though Arvinas is planning to opt for an accelerated approval based on its Phase II data readout. The landscape of mHSPC has evolved tremendously in the past decades. The treatment paradigm has shifted from androgen deprivation therapy (ADT) alone to doublet combinations comprising ADT with docetaxel or an androgen receptor inhibitor, and now triplet therapy involving all three classes of agents. Apart from XTANDI, ZYTIGA, and ERLEADA in the mCSPC market, Bayer's NUBEQA is another rising contender with a strong uptake in a short period. Bayer is further strategizing to increase the prescription by volume for NUBEQA by label expansion in patients who are not eligible for chemotherapy in the ARANOTE Phase III trial. PARP inhibitors such as AKEEGA and TALZENNA are also currently being evaluated in the mHSPC space alone and with ARIs. Novartis' radioligand therapy, PLUVICTO approved in 2022, has generated an unexpected revenue from the third-line mCRPC setting, further plans to expand in an earlier line in mCRPC by 2024 in the United States. The approval of PLUVICTO has also marked a crucial advancement in treating progressive mCRPC, offering improved survival rates for those with limited treatment options. The drug had an exceptionally robust initial market performance, garnering a stronger-than-expected uptake in the US. The drug is currently being studied in the Phase III PSMAddition study to see if that triplet combination is better than ADT and an androgen receptor signaling inhibitor alone in patients with mHSPC. Discover which therapies are expected to grab the major metastatic prostate cancer market share @ Metastatic Prostate Cancer Market Report Metastatic Prostate Cancer Overview Prostate cancer, a form of malignancy specific to the prostate gland within the male reproductive system, can advance to a metastatic stage, spreading from the prostate to other areas of the body. This advanced stage is often referred to as metastatic or advanced prostate cancer, commonly extending to lymph nodes or bones. Prostate cancer symptoms can differ widely among individuals. Although some men might not experience any symptoms, typical signs may include the presence of blood in the urine or semen, painful ejaculation, discomfort or a burning sensation during urination, and various other related symptoms. The primary diagnostic method involves prostate-specific antigen (PSA) testing, which detects elevated PSA levels in individuals affected by prostate cancer or other prostate-related conditions. Screening processes may also include a digital rectal exam to identify any notable prostate tumors, alongside additional methods such as prostate ultrasound and MRI scans. However, a conclusive diagnosis typically necessitates a transrectal ultrasound-guided (TRUS) prostate tissue biopsy. Metastatic Prostate Cancer Epidemiology Segmentation As per DelveInsight analysis, the United States had the highest number of diagnosed prostate cancer cases in 2022, with approximately 2.9 million reported cases. In 2022, total cases of metastatic CSPC/HSPC and metastatic CRPC were around 100K and 120K, respectively, in the 7MM. These cases are expected to increase by 2032. The metastatic prostate cancer market report proffers epidemiological analysis for the study period 2019–2032 in the 7MM segmented into: Total Prevalent Cases of Prostate Cancer Total Diagnosed Cases of Prostate Cancer Age-Specific Cases of Prostate Cancer Total Diagnosed Cases of Prostate Cancer by Clinical Stages Total Metastatic Cases of Prostate Cancer Total Treated Cases of mCRPC Total Treated Cases of mCSPC Metastatic Prostate Cancer Treatment Market Metastatic Castration-Resistant Prostate Cancer (mCRPC) is a stage of prostate cancer that has spread to other parts of the body, such as lymph nodes or bones, and no longer responds to treatment that lowers testosterone. Despite currently approved therapeutics, mCRPC remains a terminal diagnosis with an aggressive disease course. ADT is a stalwart therapy for the initial treatment of metastatic disease. Unfortunately, most men in this situation will go on to develop mCRPC and require secondary systemic therapy. This disease state can be very challenging to treat. Docetaxel was the only agent available for the treatment of mCRPC until 2010, which showed an increase in overall survival compared with the standard of care. It was approved in 2004 for mCRPC with prednisone. Patients failed to first-line docetaxel for many years, and no standard treatment option was approved. However, in the last few years, several drugs such as JEVTANA, ZYTIGA, XTANDI, LYNPARZA, TALZENNA, AKEEGA, and others have received regulatory approval for mCRPC in the United States. Most recently, PARP inhibitors have shown tremendous development in this area with AKEEGA (Janssen), followed by TALZENNA (Pfizer/Astellas Pharma) and LYNPARZA in combination (AstraZeneca/Merck) getting approved in mCRPC in 2023. The approval of PLUVICTO has also marked a crucial advancement in treating progressive mCRPC, offering improved survival rates for those with limited treatment options. The drug had an exceptionally robust initial market performance, garnering a stronger-than-expected uptake in the US. Quantitatively, the mCRPC pipeline seems to be quite strong. ADCs such as MGC018 and DS-7300 have both displayed encouraging results in clinical trials involving patients with mCRPC. However, except for Point Biopharma's therapy, none of these potential players have initiated a Phase III trial, even though Arvinas plans to opt for an accelerated approval based on its Phase II data readout. Metastatic Castrate-Sensitive Prostate Cancer (mCSPC) is an advanced form of cancer in which cancer cells have spread from the prostate to other body areas. However, the patient is still sensitive to androgen deprivation therapy (ADT) (some mCSPC patients have never had ADT, while others may have had ADT but have recovered testicular function). The backbone of all treatments in mCSPC is androgen deprivation therapy (ADT) with medications that suppress the level of testosterone in the body because testosterone is the fuel for prostate cancer and gives the signals to grow and spread. Studies over the last decade have demonstrated that intensification of androgen deprivation with different treatment modalities correlates with prolongation of survival. The options for intensification include docetaxel chemotherapy, different androgen receptor-targeted agents, including abiraterone acetate, apalutamide, and enzalutamide, and radiation to the prostate. Most recently, the treatment paradigm for mHSPC shifted to triplet therapy, NUBEQA combined with ADT and chemotherapy. According to the findings presented at the ASCO GU 2023, the regimen should be considered the new standard of care for this patient population. To know more about metastatic prostate cancer treatment guidelines, visit @ Metastatic Prostate Cancer Management Metastatic Prostate Cancer Pipeline Therapies and Key Companies Capivasertib (AZD 5363): AstraZeneca Bavdegalutamide (ARV-110): Arvinas MVI-816 (pTVG-HP): Madison Vaccines PT-112: Phosplatin Therapeutics HC-1119: Hinova Pharmaceuticals OPDIVO (nivolumab): Bristol Myers Squibb KEYTRUDA (Pembrolizumab/MK-3475): Merck MGC018 (vobramitamab duocarmazine): MacroGenics DS-7300: Daiichi Sankyo Ceralasertib: AstraZeneca Ladiratuzumab vedotin: Seagen/Merck BMS-986218: Bristol-Myers Squibb TAS-115: Taiho Pharmaceutical ModraDoc006/r: Modra Pharmaceuticals Vudalimab: Xencor (Lu-177) - PNT2002: Point Biopharma LNTH-1095 (MIP-1095): Lantheus Holdings ZEN-3694: Zenith Epigenetics EPI-7386: Essa Pharma 177Lu-DOTA-rosopatamab: Telix Pharmaceuticals Proxalutamide: Kintor Pharmaceutical Masitinib: AB Science VERZENIO (Abemaciclib/LY2835219): Eli Lilly and Company CABOMETYX (cabozantinib): Exelixis Learn more about the FDA-approved drugs for metastatic prostate cancer @ Drugs for Metastatic Prostate Cancer Treatment Metastatic Prostate Cancer Market Dynamics The dynamics of the metastatic prostate cancer are expected to change in the coming years. Before 2010, docetaxel was the primary therapeutic option for metastatic castration-resistant prostate cancer (mCRPC), demonstrating improved overall survival compared to the established standard of care. Its approval in 2004, alongside prednisone, marked a milestone in mCRPC treatment. Following initial docetaxel therapy failure, patients faced a dearth of approved second-line treatments for numerous years. However, recent years have witnessed regulatory approvals of multiple drugs in the United States for mCRPC, transforming the treatment landscape. Notably, medications such as JEVTANA, ZYTIGA, XTANDI, LYNPARZA, TALZENNA, AKEEGA, and several others have gained approval. Of late, significant advancements have emerged in the realm of mCRPC, particularly with PARP inhibitors. AKEEGA from Janssen, TALZENNA jointly developed by Pfizer and Astellas Pharma, and the combination of LYNPARZA by AstraZeneca and Merck garnered approval in 2023, showcasing remarkable progress in this domain. PLUVICTO's approval is a significant leap forward in the management of progressive metastatic castration-resistant prostate cancer, bringing improved survival rates to patients with limited treatment alternatives. The drug witnessed an exceptional and robust initial performance in the US market, exceeding expectations. In numerical terms, the pipeline for metastatic castration-resistant prostate cancer appears robust. Antibody-drug conjugates like MGC018 and DS-7300 have demonstrated promising outcomes in clinical trials among mCRPC patients. Nevertheless, except for Point Biopharma's treatment, the majority of these prospective treatments have yet to commence a Phase III trial. Despite this, Arvinas intends to pursue an expedited approval pathway leveraging its Phase II data for regulatory approval. Scope of the Metastatic Prostate Cancer Market Report Therapeutic Assessment: Metastatic Prostate Cancer current marketed and emerging therapies Metastatic Prostate Cancer Market Dynamics: Key Market Forecast Assumptions of Emerging Metastatic Prostate Cancer Drugs and Market Outlook Competitive Intelligence Analysis: SWOT analysis and Market entry strategies Unmet Needs, KOL's views, Analyst's views, Metastatic Prostate Cancer Market Access and Reimbursement Discover more about metastatic prostate cancer drugs in development @ Metastatic Prostate Cancer Clinical Trials Table of Contents Related Reports Prostate Cancer Epidemiology Forecast Prostate Cancer Epidemiology Forecast – 2032 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, and prostate cancer epidemiology trends. Metastatic Prostate Cancer Pipeline Metastatic Prostate Cancer Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key metastatic prostate cancer companies, including AstraZeneca, Arvinas, Madison Vaccines, Phosplatin Therapeutics, Hinova Pharmaceuticals, Bristol Myers Squibb, Merck, MacroGenics, Daiichi Sankyo, Seagen, Taiho Pharmaceutical, Modra Pharmaceuticals, Xencor, Point Biopharma, Lantheus Holdings, Zenith Epigenetics, Essa Pharma, Telix Pharmaceuticals, Kintor Pharmaceutical, AB Science, Eli Lilly and Company, Exelixis , among others. Metastatic Castration-Resistant Prostate Cancer Market Metastatic Castration-Resistant Prostate Cancer Market Insights, Epidemiology, and Market Forecast – 2032 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and key metastatic castration-resistant prostate cancer companies including AstraZeneca, Arvinas, Madison Vaccines, Phosplatin Therapeutics, Hinova Pharmaceuticals, Bristol Myers Squibb, Merck, MacroGenics, Daiichi Sankyo, Seagen, Taiho Pharmaceutical, Modra Pharmaceuticals, Xencor, Point Biopharma, Lantheus Holdings, Zenith Epigenetics, Essa Pharma, Telix Pharmaceuticals, Kintor Pharmaceutical, AB Science, Eli Lilly and Company, Exelixis among others. Metastatic Hormone-Refractory Prostate Cancer Pipeline Metastatic Hormone-Refractory Prostate Cancer Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products, and the key metastatic hormone-refractory prostate cancer companies, including AstraZeneca, Arvinas, Madison Vaccines, Phosplatin Therapeutics, Hinova Pharmaceuticals, Bristol Myers Squibb, Merck, MacroGenics, Daiichi Sankyo, Seagen, Taiho Pharmaceutical, Modra Pharmaceuticals, Xencor, Point Biopharma, Lantheus Holdings, Zenith Epigenetics, Essa Pharma, Telix Pharmaceuticals, Kintor Pharmaceutical, AB Science, Eli Lilly and Company, Exelixis, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +91-9650213330 Logo: SOURCE DelveInsight Business Research, LLP

Phase 3Drug ApprovalClinical ResultPhase 2

31 Oct 2022

·www.prnewswire.com

Hinova Disclosed the Preclinical Results of HP518 (Oral AR PROTAC) at the 5th Annual TPD Summit

BOSTON, Oct. 28, 2022 /PRNewswire/ -- Hinova Pharmaceuticals Inc. (STAR: 688302), a clinical-stage biopharmaceutical company focused on developing novel therapeutics for cancers and metabolic diseases through targeted protein degradation technologies, today presented their preclinical results of HP518, an orally bioavailable chimeric degrader targeting androgen receptor (AR) for prostate cancer treatment, at the 5th Annual TPD Summit. Discovered and developed by Hinova, HP518 showed high degradation activity against fl-AR and most enzalutamide resistant AR point mutants, and demonstrated excellent antiproliferation activities against prostate cancer cell lines. Meanwhile, HP518 exhibited good metabolic stability and is stable in human plasma. HP518 showed excellent antitumor efficacy in xenograft model by oral dosing. HP518 was also well tolerated in preclinical tox studies. HP518 is currently in Phase-I clinical trials in Australia. The ongoing open-label clinical study will evaluate the safety, pharmacokinetics, and anti-tumor activity of HP518 in patients with metastatic castration-resistant prostate cancer (mCRPC). "Existing data makes us more confident that HP518 has the potential to be an innovative clinical option to patients with mCRPC," said Xinghai Li, MD/Ph.D., Chief Science Officer of Hinova, "Considering prostate cancer is a progressive disease, we have established a strong pipeline targeting the androgen receptor pathway for prostate cancer treatment. Based on our targeted protein degradation drug discovery platform, we are committed to develop best-in-class and first-in-class medicines to address unmet medical needs." Hinova has established a targeted protein degradation drug discovery platform, which allows Hinova to integrate TPD biology and medicinal chemistry and to identify and optimize chimeric degraders with high efficiency. Furthermore, Hinova has accumulated much experience in development of Chimeric degrader. About Hinova Hinova is an international and clinical-stage biopharmaceutical company engaged in the development of innovative deuterated and chimeric degraders for cancers and metabolic diseases. The company has 4 clinical-stage programs: HC-1119, a deuterated compound of enzalutamide, for the treatment of men with mCRPC; HP501, an URAT1 inhibitor, for hyperuricemia/gout treatment；HP558, a First-in-class CD44v6 inhibitor, for esophageal cancer treatment; and HP518, an oral AR degrader, with the potential to solve the drug resistance to prostate cancer due to AR variation. For more information, visit http://www.hinovapharma.com/en/.

PROTACsFirst in ClassPre-Clinical DataPhase 1

100 Deals associated with Deuterated enzalutamide

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Castration-Resistant Prostatic Cancer	NDA/BLA	CN	Hinova Pharmaceuticals, Inc.	23 Mar 2023
Prostatic cancer metastatic	Phase 3	US	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Prostatic cancer metastatic	Phase 3	NL	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Prostatic cancer metastatic	Phase 3	FI	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Prostatic cancer metastatic	Phase 3	ES	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Prostatic cancer metastatic	Phase 3	DE	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Prostatic cancer metastatic	Phase 3	CA	Hinova Pharmaceuticals (Usa) Inc	15 Mar 2021
Metastatic castration-resistant prostate cancer	Phase 3	CN	Hinova Pharmaceuticals, Inc.	12 Apr 2019

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


HC-1119 (CSCO2022)	Not Applicable	Castration-Resistant Prostatic Cancer	43	HC-1119 软胶囊	(dnjxoeioio) = sawkmwyror babifqacku (vjfanpqcef ) View more	-	21 Sep 2022
NCT03851640 (NEWS) Manual	Phase 3	Metastatic castration-resistant prostate cancer Second line \| Third line	417	德恩鲁胺	(gedyywnflk) = 目前研究结果显示，HC-1119软胶囊治疗后的影像学无进展生存期（rPFS）达到预期并且具有显著统计学意义，可以显著降低转移性去势抵抗性前列腺癌患者的疾病进展风险 skweblyqjr (ciyticuchw )	Positive	27 Jun 2022
NCT03851640 (NEWS) Manual	Phase 3		417	Placebo		Positive	27 Jun 2022
ASCO2018	Phase 1	Neoplasms	-	HC-1119	(ddyxwzoffg) = 5% ehtscjzbrm (uqbkbnvkfn ) View more	Positive	01 Jun 2018
NCT03851640 (HC-1119-04, ASCO2023) Manual	Phase 3	Castration-Resistant Prostatic Cancer	417	Deutenzalutamide	(rxrbmqjkgl): HR = 0.58 (95% CI, 0.439 - 0.770) Met View more	Positive	26 May 2023
NCT03851640 (HC-1119-04, ASCO2023) Manual	Phase 3	Castration-Resistant Prostatic Cancer	417	placebo		Positive	26 May 2023
NCT03774056 (Pubmed \| Int J Cancer)	Phase 1	Metastatic castration-resistant prostate cancer	43	HC-1119 200 mg/day	(nfpuloflgb) = jdzampljue lxbgswmajp (ktuutrmafv )	-	10 Jun 2021

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Synapse data is also accessible to external entities via APIs or data packages. Leverages most recent intelligence information, enabling fullest potential.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis