A Randomized, Double-blind, Placebo-Controlled, Phase III Study to Evaluate the Efficacy and Safety of Proxalutamide (GT0918) in Hospitalized COVID-19 Subjects

This study is an adaptive Phase III randomized double-blind placebo-controlled trial to evaluate the efficacy and safety of Proxalutamide (GT0918) in hospitalized adults diagnosed with COVID-19. The study is a multicenter trial that will be conducted globally. The study will compare GT0918 plus standard of care (SOC) with the placebo plus SOC. Approximately 762 subjects will be randomized in a 1:1 ratio to either GT0918 plus SOC or placebo plus SOC group.

Start Date30 Sep 2021

Sponsor / Collaborator

Suzhou Kintor Pharmaceuticals, Inc.

NCT04869228 / TerminatedPhase 3

A Phase 3 Randomized, Double-Blind Placebo Controlled, Multi-regional Trial to Evaluate the Efficacy and Safety of GT0918 for the Treatment of Mild to Moderate COVID-19 Male Patients

The purpose of this study is to assess the efficacy and safety of Proxalutamide (GT0918) in male outpatients with mild to moderate COVID-19 disease

Start Date04 Aug 2021

Sponsor / Collaborator

Suzhou Kintor Pharmaceuticals, Inc.

NCT05076851 / Unknown statusPhase 2IIT

A Randomized, Controlled, Double-blind, Single Center，Clinical Trial to Evaluate the Efficacy and Safety of Neoadjuvant Therapy With Proxalutamide Combined With Androgen Deprivation Therapy（ADT）for High Risk Prostate Cancer

This trial aims to evaluate the efficacy and safety of neoadjuvant therapy with Proxalutamide combined with androgen deprivation therapy（ADT）for High risk prostate cancer ，This trial is A randomized, controlled, double-blind, single center.Treatment cycle is 6 months,

Start Date17 Jun 2021

Sponsor / Collaborator-

100 Clinical Results associated with Proxalutamide

100 Translational Medicine associated with Proxalutamide

100 Patents (Medical) associated with Proxalutamide

Literatures (Medical) associated with Proxalutamide

01 Mar 2024·International journal of antimicrobial agents

Small-molecule antiviral treatments for COVID-19: A systematic review and network meta-analysis

Review

Author: Yang, Wenjuan ; Xin, Chuanwei ; Zheng, Bei ; Han, Bing ; Ying, Yin ; Zhu, Jun ; Yang, Bo ; Zhang, Meiling ; Feng, Pinpin ; Zhao, Qinqin ; Li, Gonghua

OBJECTIVE:

This study aimed to explore the efficacy and safety of small-molecule antivirals for treating coronavirus disease 2019 (COVID-19).

METHODS:

Seven databases were searched from their inception to 01 June 2023. The risk of bias in randomised controlled trials and retrospective studies was evaluated individually using the Cochrane risk-of-bias tool and Newcastle Ottawa Scale.

RESULTS:

In total, 160 studies involving 933 409 COVID-19 patients were evaluated. Compared with placebo or standard of care, proxalutamide demonstrated remarkable efficacy in reducing mortality rates, hospitalisation rates, serious adverse events, and the need for mechanical ventilation. Furthermore, it significantly enhanced both the rate of clinical improvement and expedited the duration of clinical recovery when compared with control groups. In patients with mild-to-moderate COVID-19, proxalutamide exhibited the above advantages, except for mortality reduction. Triazavirin was the most effective treatment for reducing the time required for viral clearance and improving the discharge rate. Leritrelvir and VV116 were ranked first in terms of enhancing the viral clearance rate on days 7 and 14, respectively. Molnupiravir was the most effective treatment for reducing the need for oxygen support. Overall, these findings remained consistent across the various subgroups.

CONCLUSIONS:

A thorough evaluation of effectiveness, applicable to both mild-to-moderate and unstratified populations, highlights the specific advantages of proxalutamide, nirmatrelvir/ritonavir, triazavirin, azvudine, molnupiravir, and VV116 in combating COVID-19. Additional clinical data are required to confirm the efficacy and safety of simnotrelvir/ritonavir and leritrelvir. The safety profiles of these antivirals were deemed acceptable.

15 Aug 2023·International journal of cancer

Proxalutamide in metastatic castration-resistant prostate cancer: Primary analysis of a multicenter, randomized, open-label, phase 2 trial.

Article

Author: Fu, Cheng ; Ye, Dingwei ; Shi, Guowei ; Qin, Shengfei ; He, Dalin ; Song, Xishuang ; Meng, Qinggui ; Zhou, Tie ; Chen, Guanghua ; Hou, Jianguo ; Wang, Jingen ; Hu, Zhiquan ; Xu, Weidong ; Sun, Weibing ; Liu, Ben ; Zhang, Wei ; Gao, Xu ; Yang, Yong ; Tang, Shouyan ; Li, Song ; Wang, Dongwen ; Wang, Yinhuai ; Sun, Zhongquan ; Jin, Jie ; Chen, Lijun

We aim to assess the safety and efficacy of proxalutamide, a novel androgen receptor antagonist, for men with metastatic castration-resistant prostate cancer (mCRPC) in a multicenter, randomized, open-label, phase 2 trial. In our study, the enrolled mCRPC patients were randomized to 100, 200 and 300 mg dose groups at 1:1:1. The primary efficacy endpoint was prostate-specific antigen (PSA) response rate. The secondary endpoints included objective response rate (ORR), disease control rate (DCR) and time to PSA and radiographic progression. Safety and pharmacokinetics were also assessed. Finally, there were 108 patients from 17 centers being enrolled. By week 16, there were 13 (35.1%), 12 (36.4%) and 15 (42.9%) patients with confirmed 50% or greater PSA decline in 100 mg (n = 37), 200 mg (n = 33) and 300 mg (n = 35) groups, respectively. Among the 19 patients with target lesions at study entry, three (15.8%) had a partial response and 12 (63.2%) had stable disease. The ORRs of 20.0%, 22.2%, 0% and DCRs of 80.0%, 88.9%, 60.0% were, respectively, achieved in 100, 200 and 300 mg groups. By the maximum follow-up time of 24 weeks, there were 42.6% and 10.2% of cases experiencing PSA progression and radiographic progression, respectively. Overall, adverse events (AEs) were experienced by 94.4% of patients, most of which were mild or moderate. There were 28 patients experiencing ≥grade 3 AEs. The most common AEs were fatigue (17.6%), anemia (14.8%), elevated AST (14.8%) and ALT (13.0%), decreased appetite (13.0%). These findings preliminarily showed the promising antitumor activity of proxalutamide in patients with mCRPC with a manageable safety profile. The proxalutamide dose of 200 mg daily is recommended for future phase 3 trial (Clinical trial registration no. CTR20170177).

25 Jul 2023·Proceedings of the National Academy of Sciences of the United States of AmericaQ1 · CROSS-FIELD

Proxalutamide reduces SARS-CoV-2 infection and associated inflammatory response.

Q1 · CROSS-FIELD

Article

Author: He, Tongchen ; Su, Fengyun ; Cheng, Caleb ; Parolia, Abhijit ; Wang, Rui ; Zhou, Qianxiang ; Ellison, Stephanie J ; Wotring, Jesse W ; Zhang, Charles J ; Zhang, Yuping ; Wang, Yini ; Yan, Honghua ; Sexton, Jonathan Z ; Zheng, Yang ; Qiao, Yuanyuan ; Ma, Liandong ; Pretto, Carla D ; Qin, Jun ; Chinnaiyan, Arul M ; Cao, Xuhong ; Jiang, Xia ; Eyunni, Sanjana

Early in the COVID-19 pandemic, data suggested that males had a higher risk of developing severe disease and that androgen deprivation therapy might be associated with protection. Combined with the fact that TMPRSS2 (transmembrane serine protease 2), a host entry factor for the SARS-CoV-2 virus, was a well-known androgen-regulated gene, this led to an upsurge of research investigating androgen receptor (AR)-targeting drugs. Proxalutamide, an AR antagonist, was shown in initial clinical studies to benefit COVID-19 patients; however, further validation is needed as one study was retracted. Due to continued interest in proxalutamide, which is in phase 3 trials, we examined its ability to impact SARS-CoV-2 infection and downstream inflammatory responses. Proxalutamide exerted similar effects as enzalutamide, an AR antagonist prescribed for advanced prostate cancer, in decreasing AR signaling and expression of TMPRSS2 and angiotensin-converting enzyme 2 (ACE2), the SARS-CoV-2 receptor. However, proxalutamide led to degradation of AR protein, which was not observed with enzalutamide. Proxalutamide inhibited SARS-CoV-2 infection with an IC₅₀ value of 97 nM, compared to 281 nM for enzalutamide. Importantly, proxalutamide inhibited infection by multiple SARS-CoV-2 variants and synergized with remdesivir. Proxalutamide protected against cell death in response to tumor necrosis factor alpha and interferon gamma, and overall survival of mice was increased with proxalutamide treatment prior to cytokine exposure. Mechanistically, we found that proxalutamide increased levels of NRF2, an essential transcription factor that mediates antioxidant responses, and decreased lung inflammation. These data provide compelling evidence that proxalutamide can prevent SARS-CoV-2 infection and cytokine-induced lung damage, suggesting that promising clinical data may emerge from ongoing phase 3 trials.

News (Medical) associated with Proxalutamide

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

30 Mar 2023

·www.biospace.com

Kintor Pharma Announces 2022 Annual Results and Recent Business Progress

SUZHOU, China, March 30, 2023 /PRNewswire/ -- Kintor Pharmaceutical Limited (Kintor Pharma, HKEX: 9939), a clinical-stage biotechnology company developing innovative small molecules and biological therapeutics, today announced business highlights and financial results for the year ended 31 December 2022. Business Highlights Kintor Pharma has made rapid progress on global clinical development, and achieved positive data read-outs of core products during the reporting period. Kintor Pharma has rolled out the clinical pipeline in dermatology area globally. Kintor Pharma is actively promoting the business development opportunities in China and globally to accelerate the commercialization progress. Kintor Pharma has raised about $100 million through 2 top-up placements during the reporting period. The company's stock has been included in MSCI China Index and Shanghai-Hong Kong Stock Connect, which increased the stock's liquidity in the capital market. The company's R&D outcome has been accepted by reputable academic conferences including AACR, ASH and AAD of the U.S., which has demonstrated its R&D capabilities. Dr. Youzhi Tong, founder, Chairman, and CEO of Kintor Pharma, commented, 2022 has been a challenging year for the global biotech industry. Under the difficulty market conditions, Kintor Pharma has made rapid progress in R&D, financing and academic publications. In terms of R&D, the company has made steady progress in its pipeline and achieved positive data read-outs of its core products, including Pyrilutamide (KX-826) for androgenetic alopecia (AGA) indication, GT20029 for AGA and acne vulgaris indications. The Phase II clinical trials of KX-826 for male and female AGA in China have reached the primary endpoints, respectively. Kintor Pharma has rolled out the clinical pipeline in dermatology area globally, and is actively promoting the business development opportunities in China and globally to accelerate the commercialization progress. In capital market, the company has raised net proceeds of $100 million through two top-up placements during the reporting period. In addition, the company's stock has been included in the MSCI China Index and the Shanghai-Hong Kong Stock Connect, further enhanced the stock's liquidity in the capital market. In academics, the company's research results have been presented at important academic conferences such as AACR, ASH and AAD of the U.S., proving that the company's innovation ability and its international influence. Looking forward, Kintor Pharma will continue to execute the development of the core products in China and globally, expecting to accelerate its commercialization process. The company strives to bring safe and effective therapeutics to the patients around the globe, and create value for its shareholders and employees. Rapid Progress on Global Clinical Development and Positive Data Read-outs of Core Products As a Biotech company focusing on the R&D and industrialization of potential First-in-Class and Best-in-Class innovative drugs, Kintor Pharma has developed a diversified product pipeline including small-molecule drugs, biologics innovative drugs and combination therapies. At present, the company has seven novel drug candidates with First-in-Class or Best-in-Class potential in Phase I-III clinical stages in China and around the world. Since 2022, the company has released positive clinical results of core products, including the Phase II clinical trials of KX-826 for male and female AGA in China, respectively, and the Phase I clinical trials of GT20029 for the treatment of AGA and ance in both China and the U.S.. Pyrilutamide (KX-826) is a topical androgen receptor (AR) antagonist that is under clinical development for the potential treatment of AGA and acne. KX-826 is the world's first AR antagonist for AGA treatment which entered the Phase III clinical trial stage. On 27 August 2022, one of the leading principal investigators of the Phase II clinical trial of KX-826 in China for the treatment of male AGA adults, Professor Jianzhong Zhang (张建中) from Peking University People's Hospital, released the trial's positive results at the 6th Annual Meeting of Chinese Hair Research Society (第六届全国毛发学术会议). The results showed that after 24 weeks of treatment, the non-vellus target area hair counts (TAHC) in the 5mg (0.5% concentration) twice daily (BID) KX-826 group increased by 15.34/cm2 compared with the placebo group from baseline, with a statistical difference (P=0.024). On 1 December 2022, the company announced that the primary endpoint of Phase II clinical trial of KX-826 for female AGA adults in China was met. After 24 weeks of treatment, the non-vellus TAHC in the 5mg (0.5% concentration) once daily (QD) KX-826 group increased by 11.39/cm2 compared with the placebo group from baseline, with a statistical difference (P=0.0087). KX-826 has showed a good safety pro both trials. GT20029 is a topical AR-Proteolysis Targeting Chimera (PROTAC) compound that is under clinical development for the potential treatment of AGA and acne. GT20029 is the world's first topical PROTAC compound which entered the clinical stage. On 24 November 2022, the company announced the top-line data of the Phase I clinical trial of GT20029 for the treatment of AGA and acne in China. The results showed that GT20029 demonstrated good safety, tolerability and pharmacokinetics in healthy subjects. On 10 February 2023, the company announced the top-line data of the Phase I clinical trial of GT20029 for the treatment of AGA and acne in the U.S.. The results showed that GT20029 demonstrated good safety, tolerability and pharmacokinetics following topical single ascending dose (SAD) administration in healthy subjects and multiple ascending dose (MAD) administration in subjects with AGA or acne. In addition, the company's product pipeline includes Pruxelutamide, GT1708F, GT0486, ALK-1 antibody (GT90001) and GT90008 in the clinical stage, and c-Myc inhibitor, compound of other targets out of PROTAC platform and ALK-1/VEGF bispecific antibody in the preclinical stage. The company's Hedgehog/SMO inhibitor GT1708F is being explored for both idiopathic pulmonary fibrosis (IPF) indication and combination therapy in blood cancer. The company is now preparing for clinical trial application for the IPF indication. The Growing Visibility in the Capital Market Since its listing on the Hong Kong Stock Exchange on 22 May 2020, the company's development has received long-term support from investors around the world. In 2022, the company successfully completed two top-up placements in the capital market and raised about $100 million. After being included in the Hong Kong Stock Connect program in September 2021, the company's stock has been included in the Shanghai-Hong Kong Stock Connect in March 2023, further expanding the company's mainland investor pool, improving its liquidity and the market influence. Thus benefits the company's future development prospects. In addition, Kintor Pharma's stock have been included in the MSCI China Index during the reporting period. Increasing Presence in Reputable Academic Seminars and Conferences Since 2022, Kintor Pharma's R&D outcome has been accepted by reputable academic conferences and journals, proving that the company's innovation ability and its international influence, and further demonstrating the First-in-Class and Best-in-Class potential of the company's product pipeline. Kintor Pharma's KX-826 and GT20029 for treatment of AGA and acne presented at AAD 2023 Kintor Pharma's Hedgehog/SMO inhibitor GT1708F for the treatment of Acute Myeloid Leukemia (AML) presented at AACR 2023 Oral Presentation highlighting the data from novel dual c-Myc/GSPT1 degrader GT19715 at ASH 2022 Pruxelutamide for treatment of COVID-19 and a c-Myc degrader for treatment of blood cancer and small cell lung cancers (SCLC) presented at AACR 2022 The study result of GT19715, a novel dual-target degrader of C-Myc/GSPT1, was published in the journal Clinical Lymphoma, Myeloma & Leukemia The study result of the Phase Ib clinical trial of Pruxelutamide for treatment of breast Cancer was published in the European Journal of Cancer (EJC) Industry and Capital Market Awards Kintor Pharma's persistent efforts in R&D has been widely recognized in the industry and has won many industry and capital market awards. Top 15 Biotech of the Top 100 Hong Kong Listed Companies Top 10 Innovative Pharmaceutical Companies in 2022 R&D Innovation Outstanding Contribution Award in 2021 Top 20 Biomedical Innovation Potential List in 2022 TOP 30 Innovative Small Molecule Pharmaceutical Companies in China in 2021 TOP 20 Most Influential Small Molecule Pharmaceutical Innovation Companies in 2022 Jishi Cup Top 10 Pharmaceutical Innovation Companies in 2021 Most Valuable Pharmaceutical and Medical Companies Other Business Updates In August 2022, Dr. Lu Qun, our Chief Technology Officer, was elected as a "2022 Gusu Innovation and Entrepreneurship Leading Talent". In May 2022, the company has received the approval to set up a Doctors workstation in Guangdong Province by the Human Resources and Social Security Department of Guangdong Province. Financial Highlights As of 31 December 2022, the company's research and development costs increased by RMB828 million, up by 7.8%, from RMB767.9 million for the year ended 31 December 2021. The increased R&D costs were mainly attributable to the ongoing Phase III clinical trials, including those of Pruxelutamide for the indication of COVID-19 and mCRPC, and KX-826 for the indication of AGA during the reporting period. The company had cash and cash equivalents and time deposits of RMB875.3 million as at 31 December 2022, including utilised bank facilities of RMB 276.5 million. In addition, the company also had unutilised bank facilities of RMB 120.0 million as at 31 December 2022. The company has sufficient cash on hand to support the advancement of the clinical trials and R&D. *For more details, please refer to the 2022 annual results announcement. About Kintor Pharmaceutical Limited Kintor Pharmaceutical Limited is developing and commercializing a robust pipeline of innovative small molecule and biological therapeutics for androgen-receptor-related disease areas with unmet medical needs, including COVID-19, prostate, breast and liver cancers, alopecia and acne. For more information, visit . Company Codes: HongKong:9939

Phase 1Clinical ResultPhase 2Financial Statement

29 Sep 2022

·www.biospace.com

Kintor Pharma Announces Publication of Phase Ib Data from Pruxelutamide for AR+ mBC in EJC

SUZHOU, China, Sept. 29, 2022 /PRNewswire/ -- Kintor Pharmaceutical Limited ("Kintor Pharma", HKEX: 9939), a clinical-stage biotechnology company developing innovative small molecules and biological therapeutics, today announced that the results from a phase Ib study of pruxelutamide (used to be called proxalutamide, GT0918) for the treatment of patients with androgen receptor positive (AR+) metastatic breast cancer (AR+ mBC) in China have been published in the international journal, European Journal of Cancer (2021 Impact Factor: 10.002, EJC) on September 28, 2022, further demonstrating the efficacy and safety of pruxelutamide in patients with AR+ mBC. Highlights Pruxelutamide showed promising activity in heavily pretreated AR+ mBC patients. Pruxelutamide showed an acceptable safety pro heavily pretreated AR+ mBC. Recommended phase II dose of pruxelutamide was defined as 200mg orally once daily. AR expression, cell-free DNA yield, CNV might be associated with response. Patients with PIK3CA pathogenic mutation showed longer progression-free survival. Metastatic breast cancer (mBC) remains a largely incurable disease in most patients, resulting in approximately 0.5 million deaths every year worldwide. At present, the primary goals of mBC therapy are to prolong patient survival and maintain their quality of life. Any novel therapy likely to provide a survival advantage in patients is valuable. Pruxelutamide is an oral, newly-generation AR antagonist, developed by Kintor Pharma. Results from this study of pruxelutamide were published in a paper titled "Proxalutamide in patients with AR-positive metastatic breast cancer: Results from an open-label multicentre phase Ib study and biomarker analysis". This phase Ib study was designed to evaluate the preliminary efficacy and safety of pruxelutamide monotherapy in patients with pretreated AR+ mBC and to determine the RP2D of pruxelutamide. The corresponding author of the paper, Professor Huiping Li of Peking University Cancer Hospital & Institute, was the principal investigator of the phase I clinical trial in China. In this open-label, dose-expansion, multicentre phase Ib trial, patients with AR+ mBC (immunohistochemistry [IHC] AR≥1%) received pruxelutamide orally once daily. Two pruxelutamide dose cohorts (cohort A: 200mg; cohort B: 300mg) were sequentially investigated. Primary endpoints were disease control rate (DCR) at 8 and 16 weeks and recommended phase II dose (RP2D). Finally, 45 eligible patients were enrolled and treated. 30 eligible patients were enrolled in cohort A (200mg orally once daily) from April 19, 2018, to March 7, 2019. 15 patients were enrolled into cohort B (300mg orally once daily) from March 11, 2019, to April 16, 2019. Among 39 evaluable patients, DCR at 8 and 16 weeks was 25.6% (95% confidence interval [CI], 11.9–39.4%), with 26.9% in cohort A and 23.1% in cohort B. The 6-month progression-free survival (PFS) rate was 19.6% (95% CI, 10.2–37.5%). In the triple-negative subgroup, DCR at 8 weeks was 38.5%, with median PFS of 9.1 months (95% CI, 7.8–NA) in those who achieved response at 8 weeks (n = 5). All 45 patients were evaluable for safety. Overall, pruxelutamide demonstrated a good safety profile. The most common grade 3 or 4 AEs were AST increase (8.9%) and γ-glutamyltransferase increase (8.9%). No treatment-related deaths or dose reductions occurred in either cohort. This study conducted another exploratory analysis to identify potential predictive biomarkers of treatment response. By biomarker analysis, patients with moderate AR expression of IHC (26%–75%), PIK3CA pathogenic mutations, or <60 ng/ml cell-free DNA yield showed longer PFS. In conclusion, pruxelutamide demonstrated promising anti-tumour activity with an acceptable safety pro patients with heavily pretreated AR+ mBC, particularly in the TNBC subgroup. And, this study determined the RP2D to be 200mg orally once daily. Furthermore, we identified that AR expression, CNVs, and cfDNA yield may be associated with the response to pruxelutamide, highlighting the importance of conducting genomic profiling in patients with AR+ mBC to identify those likely to benefit from pruxelutamide treatment. The data supports further clinical development of pruxelutamide on treating breast cancer patients. About Kintor Pharmaceutical Limited Kintor Pharmaceutical Limited is developing and commercializing a robust pipeline of innovative small molecule and biological therapeutics for androgen-receptor-related disease areas with unmet medical needs, including COVID-19, prostate, breast and liver cancers, alopecia and acne. For more information, visit . View original content: SOURCE Kintor Pharma Company Codes: HongKong:9939

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100 Deals associated with Proxalutamide

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
COVID-19	PY	Suzhou Kintor Pharmaceuticals, Inc.	16 Jul 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Severe Acute Respiratory Syndrome	Phase 3	BR	Sutro Biopharma, Inc.	02 Feb 2021
Metastatic castration-resistant prostate cancer	Phase 3	CN	Suzhou Kintor Pharmaceuticals, Inc.	30 Apr 2019
Metastatic castration-resistant prostate cancer	Phase 3	CN	China Pharmaceutical University	30 Apr 2019
Metastatic breast cancer	Phase 2	CN	Suzhou Kintor Pharmaceuticals, Inc.	27 Apr 2023
Castration-Resistant Prostatic Cancer	Phase 2	US	Suzhou Kintor Pharmaceuticals, Inc.	30 May 2019
Hormone receptor positive breast cancer	Phase 1	CN	Suzhou Kintor Pharmaceuticals, Inc.	18 Jun 2019
Hormone receptor positive breast cancer	Phase 1	CN	China Pharmaceutical University	18 Jun 2019
Prostatic cancer metastatic	Phase 1	US	Suzhou Kintor Pharmaceuticals, Inc.	10 Feb 2016

Clinical Result

Indication

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03899467 (CTgov)	Phase 2	Metastatic castration-resistant prostate cancer	61	GT0918 (Arm 1: 400 mg /Day of GT0918)	mqufjvarlg(fmjmhuugnl) = vbzqdenrsm dokjzbifvy (hyellgldly, jocejusxye - gupmnymxxu) View more	-	02 Jan 2024
				GT0918 (Arm 2: 500 mg/Day of GT0918)	mqufjvarlg(fmjmhuugnl) = rxidvplsht dokjzbifvy (hyellgldly, kcoumwsxpg - frppbbvyhf) View more
SABCS2023	Not Applicable	Metastatic breast cancer First line HR+ \| HER2- \| AR+	38	Proxalutamide plus Fulvestrant	vojorwxbiq(eltvpjaiko) = agomeabusx qynbuaknkv (fupazrvqxo, 3.2% - 37.9%) View more	-	05 Dec 2023
CTR20191063 (ESMO2023) Manual	Phase 1	AR Positive/ER Positive/HER2 Negative Breast Cancer HR positive \| HER2 negative \| AR positive	37	proxalutamide plus fulvestrant	hhxglgrrpu(btgzidecrb) = ecxthwkxtz zymdwkivif (ghtekuqnmg ) View more	Positive	21 Oct 2023
				proxalutamide plus fulvestrant (part 1)	efsuawhfpf(dvienqdcrv) = lqitfihqbz tolbiiagtm (kkenfkybga ) View more
NCT04103853 \| CTR20170757 (Pubmed)	Phase 1	Metastatic breast cancer	63	Proxalutamide 200 mg	jduejsmyag(bwaxrcvfbx) = tewnyshiqi igqxxwpwjr (efpalusvmt, 11.9 - 39.4) View more	-	28 Sep 2022
				Proxalutamide 300 mg	jduejsmyag(bwaxrcvfbx) = zmxoawjfjn igqxxwpwjr (efpalusvmt, 11.9 - 39.4) View more
NCT04870606 (MRCT, NEWS) Manual	Phase 3	COVID-19	733	Standard of Care+Proxalutamide	ofudfgtuux(ckotulqcsr) = reduced the risk of hospitalization/death by100% ijnlksrato (ttwerqqtrt ) View more	Positive	06 Apr 2022
				Standard of Care+Placebo
NCT04728802 \| NCT05126628 (Pubmed) Manual	Phase 3	COVID-19	778	Proxalutamide	vatmzwyodv(yrhjvqeplv) = ckfnevzxak sqslugmgzq (geqttampvt ) View more	Positive	25 Dec 2021
				Placebo	vatmzwyodv(yrhjvqeplv) = qkjrbkedny sqslugmgzq (geqttampvt ) View more
CSCO2021	Phase 2	Metastatic castration-resistant prostate cancer	108	GT0918 therapy, 100 mg/day	hukijscvdz(hqgutsgcdr) = qgudperabo wxrcltpxlg (zvoixjqbls, 240 - 477) View more	-	25 Sep 2021
CSCO2021	Phase 2	Metastatic castration-resistant prostate cancer	61	GT0918	kjfawguwkg(pzuniunxvq) = vomaytzyvt xctzcxhbeg (qgukmjewta, 99.5 - 150)	-	25 Sep 2021
NCT04446429 (Pubmed \| Front Med (Lausanne)) Manual	Phase 2	COVID-19	268	proxalutamide	(luffnkoano) = ykmmcuzoca oukrdypfix (rshigbkhyw )	Positive	19 Jul 2021
				Placebo	(luffnkoano) = ltdlbomsym oukrdypfix (rshigbkhyw ) View more
NCT04728802 (CTgov)	Phase 3	Severe Acute Respiratory Syndrome \| COVID-19	645	Proxalutamide (Proxalutamide + Usual Care)	vxfmupzuqt(xpqilunlsh) = slrmzbblgt hczrrieusx (lpxadusycj, gvlqbcknbc - jwnjmpbavo) View more	-	23 Jun 2021
				placebo (Placebo + Usual Care)	vxfmupzuqt(xpqilunlsh) = rnoltpujiu hczrrieusx (lpxadusycj, lnzkkmvgwo - owbwmrlcyl) View more

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