Neratinib maleate

LOS ANGELES--(BUSINESS WIRE)-- Puma Biotechnology, Inc. (NASDAQ: PBYI), a biopharmaceutical company, announced that clinical data on neratinib were presented in a poster session at the American Association for Cancer Research (AACR) Annual Meeting 2025. The AACR Annual Meeting is currently taking place at the McCormick Place in Chicago, Illinois. The poster is entitled, “CT071: Phase I trial of trastuzumab deruxtecan in combination with neratinib in solid tumors with HER2 alterations (NCI 10495).” Andrew A. Davis, Assistant Professor at Washington University School of Medicine, presented the poster during Session PO.CT01.01 – First-in-Human Phase I Clinical Trials 1. NCI 10495 is sponsored by the National Cancer Institute, part of National Institutes of Health, and conducted in the NCI funded Experimental Therapeutics Clinical Trials Network (ETCTN). This open label, multi-center, Phase I clinical trial (NCT05372614) enrolled 20 patients in three cohorts treated with three increasing dose levels, or a 3+3 trial design, to evaluate the safety and tolerability of trastuzumab deruxtecan (T-DXd or ENHERTU®) in combination with neratinib (NERLYNX®). Eligible patients had advanced solid tumors with HER2 immunohistochemistry 3+ (IHC3+), HER2 amplification identified by in situ hybridization or next-generation sequencing, or an activating HER2 mutation. Prior treatment with trastuzumab deruxtecan was not allowed. The dose of trastuzumab deruxtecan was fixed at 5.4 mg/kg. The three dose levels (DLs) for neratinib all started at 120 mg daily for the first week. DL1 remained at 120 mg daily throughout the course of treatment, DL2 escalated to 160 mg daily in week 2 and 200 mg by week 3, and DL3 escalated to 160 mg in week 2 and 240 mg by week 3. The primary endpoints were the determination of the dose-limiting toxicities (DLTs) during the first two cycles of treatment (42 days) and the determination of the recommended Phase II dose of the combination of trastuzumab deruxtecan and neratinib. Twenty patients received study treatment (DL1 N=7, DL2 N=4, and DL3 N=9). The most common treatment-emergent adverse events of any grade included nausea (N=15, 75%), diarrhea (N=15, 75%), fatigue (N=13, 65%), and hypokalemia (N=11, 55%). Grade 3 treatment-emergent adverse events that occurred in more than 2 patients included anemia (N=6, 30%), diarrhea (N=4, 20%), and hypokalemia (N=3, 15%). The only Grade 4 treatment-related adverse event was neutropenia that occurred in 1 patient (5%). One DLT (acute kidney injury) was observed at DL1, 0 DLTs were observed in DL2, and 1 DLT was observed (fatigue leading to early drug discontinuation) at DL3. Three patients developed Grade 1 pneumonitis or interstitial lung disease (ILD), 2 at DL1 and 1 at DL3. The proportion of reported treatment-emergent adverse events was lower at higher dose levels. Of 15 response-evaluable patients by RECIST v1.1, 4 patients had a partial response (PR), including patients with gastroesophageal (N=2, one HER2 IHC 3+ and one HER2 mutated), pancreatic (N=1, IHC 3+), and ovarian (N=1, IHC 3+; unconfirmed response) cancers. Notably, 3 of 5 patients with advanced pancreatic cancer were observed to have tumor regression (1 PR for 13+ cycles, 2 with stable disease consisting of one patient with -29.4% tumor regression for 9 cycles and one patient with -13.3% tumor regression for 8 cycles). Dose level 3, which consisted of trastuzumab deruxtecan at 5.4 mg/kg and neratinib at 120 mg in week 1, 160 mg week 2, and 240 mg week 3 onward, was selected as the recommended Phase II dose. Part 2 of this study, which consists of a pharmacodynamic evaluation of trastuzumab deruxtecan (5.4 mg/kg) and neratinib (RPD2) in 12 patients, opened to enrollment in March 2025. Patients with any advanced solid tumor and HER2 amplification/overexpression or a HER2 mutation will be enrolled. “Neratinib and trastuzumab deruxtecan showed impressive combination activity in preclinical models of HER2-mutated breast cancers, which prompted evaluation of the combination in this first-in-human clinical trial. I am pleased to report that the combination not only had a manageable safety profile, but we also observed early signs of efficacy across a variety of HER2-altered tumors,” said Dr. Davis. Alan H. Auerbach, Chief Executive Officer and President of Puma Biotechnology, added, “We are pleased with the tolerability and potentially promising signals of efficacy of neratinib in combination with trastuzumab deruxtecan, especially in hard-to-treat tumors including pancreatic cancer. We look forward to continued evaluation of this combination in the Phase II portion of this study.” NCI 10495 is also supported by Puma Biotechnology and Daiichi Sankyo, Inc. through Cooperative Research and Development Agreements with NCI. Trastuzumab deruxtecan is a specifically engineered HER2 directed DXd antibody drug conjugate (ADC) discovered by Daiichi Sankyo (TSE: 4568) and being jointly developed and commercialized by Daiichi Sankyo and AstraZeneca (LSE/STO/Nasdaq: AZN). About Puma Biotechnology Puma Biotechnology, Inc. is a biopharmaceutical company with a focus on the development and commercialization of innovative products to enhance cancer care. Puma in-licensed the global development and commercialization rights to PB272 (neratinib, oral) in 2011. Neratinib, oral was approved by the U.S. Food and Drug Administration in 2017 for the extended adjuvant treatment of adult patients with early stage HER2-overexpressed/amplified breast cancer, following adjuvant trastuzumab-based therapy, and is marketed in the United States as NERLYNX® (neratinib) tablets. In February 2020, NERLYNX was also approved by the FDA in combination with capecitabine for the treatment of adult patients with advanced or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting. NERLYNX was granted marketing authorization by the European Commission in 2018 for the extended adjuvant treatment of adult patients with early stage hormone receptor-positive HER2-overexpressed/amplified breast cancer and who are less than one year from completion of prior adjuvant trastuzumab-based therapy. NERLYNX® is a registered trademark of Puma Biotechnology, Inc. In September 2022, Puma entered into an exclusive license agreement for the development and commercialization of the anti-cancer drug alisertib, a selective, small molecule, orally administered inhibitor of aurora kinase A. Initially, Puma intends to focus the development of alisertib on the treatment of small cell lung cancer and breast cancer. In February 2024, Puma initiated ALISCA™-Lung1, a Phase II clinical trial of alisertib monotherapy for the treatment of patients with extensive-stage small cell lung cancer. In November 2024, Puma initiated ALISCA™-Breast1, a Phase II clinical trial of alisertib in combination with endocrine therapy for the treatment of patients with HER2-negative, HR-positive metastatic breast cancer. Further information about Puma Biotechnology may be found at https://www.pumabiotechnology.com. Alan H. Auerbach or Mariann Ohanesian, Puma Biotechnology, Inc., +1 424 248 6500 info@pumabiotechnology.com ir@pumabiotechnology.com David Schull or Olipriya Das, Russo Partners, +1 212 845 4200 david.schull@russopartnersllc.com olipriya.das@russopartnersllc.com

SHANGHAI, April 18, 2025 /PRNewswire/ -- Asieris Pharmaceuticals today released its 2024 Annual Report, highlighting a bold and determined journey forward. With a specialty pharma strategy and operational efficiency, the company exceeded its commercialization targets and advanced its innovative products — APL-1702 and APL-1706 (Hexvix®) — toward market launch. R&D efforts also gained strong momentum, with 12 products in the pipeline and 16 ongoing research projects. As of the end of the reporting period, Asieris held approximately RMB 1.89 billion in cash, cash equivalents, and trading financial assets, providing a solid foundation for continued growth. Revenue Tops RMB 200M in 1st Year of Commercialization, with the specialized commercialization platform poised for action 2024 marked Asieris' first full year of commercialization. The company has made strides in refining market strategies and ensuring high-quality execution, while effectively managing costs and expenses. Asieris posted operating revenue of RMB 202 million, demonstrating robust growth and successfully reaching break-even targets in commercial operations. During the reporting period, the company's two commercialized products, Ouyoubi and Dipaite, saw strong uptake, reaching over 1,000 and 500 target hospitals respectively. Sales grew rapidly, with Ouyoubi capturing 27% of the neratinib tablet market and Dipaite securing 12% of the pazopanib tablet market. To further strengthen its presence in key focus areas, the company introduced multiple products and established sales partnerships in women's health and genitourinary (GU) tumors. In March 2025, it licensed-in the eribulin mesylate injection, a novel microtubule inhibitor for the treatment of advanced breast cancer. With this addition, the company's breast cancer portfolio now covers both early and late-stage disease. To further enhance commercialization efficiency, the company has launched its Commercial Operation 2.0 — building on past successes to create a leaner, more agile operating model. Key initiatives include appointing a seasoned Chief Commercial Officer to lead the function end-to-end; streamlining the organizational structure and strengthening commercial capabilities; and strategically expanding the team in line with priority areas and product launch timelines. The company has also set clear five-year business targets, including accelerating growth for existing products, preparing for the commercial rollout of Hexvix® and APL-1702, introducing new products within core therapeutic areas, maximizing synergies across the pipeline, and driving sales efficiency to the next level. Accelerating product launches to build momentum for sales In women's health, APL-1702, a combination of drug and medical device designed for photodynamic non-surgical treatment of cervical high-grade squamous intraepithelial lesions (HSIL), is making steady progress toward market approval. In May 2024, the product's marketing application was officially accepted by the National Medical Products Administration (NMPA). As of the report's release, the Center for Drug Evaluation (CDE), NMPA had completed the first round of technical reviews, covering toxicology, clinical data, biostatistics, clinical pharmacology, and pharmaceutical quality. During the reporting period, the Inspection Center also wrapped up its Good Clinical Practice (GCP) inspection. The company has since received written feedback and is actively coordinating its responses to help expedite the review process and bring APL-1702 one step closer to approval. As a first-in-class treatment set to debut in China, APL-1702 is on track to become the world's first non-invasive therapy for HSIL — supported by robust clinical evidence and validated through an international Phase III trial. Experts note that, with China facing demographic pressures and a rising incidence of cervical intraepithelial neoplasia (CIN) among younger women, surgical excision of the cervix poses increasing challenges — especially during the critical period of fertility preservation. APL-1702 is expected to bridge this critical treatment gap and contribute to the creation of a more fertility-friendly healthcare landscape. To drive the commercialization of APL-1702, the company has hosted eight expert advisory meetings, focusing on Phase III clinical data, the current landscape of HSIL diagnosis and treatment, and unmet clinical needs. These sessions earned strong endorsement from leading gynecological and pharmaceutical experts, who recognized the innovation and clinical value APL-1702 brings to the table. The company has also made meaningful progress in building strategic partnerships with government agencies and leading academic associations. In collaboration with the Cancer Foundation of China, the company unveiled the first real-world showcase of its innovative cervical cancer prevention and control system at the 7th China International Import Expo (CIIE). It also signed medium- to long-term strategic cooperation agreements with both the China Women's Development Foundation and the Cancer Foundation of China during the event. The partnerships are set to roll out in 2025. The Women's Health Division has conducted extensive market and industry research, gaining deep insights into the needs of doctors and patients and broader commercial landscape. Based on this analysis, the team has finalized key launch strategies and mapped out a commercialization roadmap, laying the groundwork for a swift market rollout once approval is secured. Given the relative scarcity of innovation in the gynecological field, APL-1702 stands out as a meaningful breakthrough, backed by solid clinical evidence and proven efficacy. The company will continue to prioritize APL-1702 and its photodynamic drug-device combination platform, in a bid to build a comprehensive, tiered gynecological portfolio. This strategy will center on product iteration and indication expansion, while leveraging synergies across the pipeline to drive broader growth. In urological tumors, after the marketing application for Hexvix® was accepted in November 2023, the company's dynamic and highly skilled team sprang into action to support the review and approval process. As a result, Hexvix® received NMPA approval in November 2024, seven months ahead of the expected timeline. The product has since made history as the first diagnostic imaging agent approved in China for photodynamic blue light cystoscopy in bladder cancer detection. The Oncology Business Unit is fine-tuning the launch strategy for Hexvix®, initially targeting patients with commercial insurance or those willing to pay out-of-pocket. The early rollout will cover the special and international medical departments of top-tier hospitals in major cities, as well as premium foreign-invested and private urology specialty hospitals. As clinical guidelines are released and endorsements from leading urology experts are established, the launch will be paired with the introduction of disposable blue light cystoscopes. Together, these efforts aim to accelerate the adoption of blue light cystoscopy in general hospitals and foster an integrated approach to the diagnosis and treatment of bladder cancer. Focusing on strategic expansion in key areas and fast-tracking high-impact R&D initiatives Aligned with its strategic vision, Asieris has made significant strides in clinical development in 2024, with its global clinical initiatives progressing efficiently. In the fields of women's health, breast cancer, and gynecological tumors, Asieris has made remarkable progress. Building on the strong results of the international multicenter Phase III study of APL-1702, the company received feedback from its communication meeting with the U.S. FDA in December 2024, culminating in an agreement on a new Phase III clinical design to support the U.S. launch of APL-1702. Asieris is now actively seeking international partners to advance the U.S. Phase III clinical trial application. Additionally, APL-1702 is also being investigated for its potential in HPV virus clearance. Meanwhile, the U.S. FDA and China's NMPA approved the Phase I/IIa clinical trial applications for APL-2302 (a USP1 small molecule inhibitor) in advanced solid tumors in October 2024 and January 2025, respectively, with the first patient enrolled in Phase Ia in March 2025. Progress on APL-2501 (CLDN6/9 ADC) is also on track, with its preclinical research and unique linker platform selected for a poster presentation at the 2025 American Association for Cancer Research Annual Meeting (AACR 2025). In the field of urologic oncology, the Phase II clinical trial of oral APL-1202 in combination with tislelizumab as a neoadjuvant therapy for muscle-invasive bladder cancer (MIBC) was successfully completed in September 2024, delivering encouraging efficacy signals. Among protocol-eligible patients, the pathological complete response (pCR) rates were 41% for the combination arm versus 20% for monotherapy. The combination was particularly effective in patients with low PD-L1 expression, where it achieved a pCR rate of 42% compared to just 11% with monotherapy. Meanwhile, APL-2401 — a dual FGFR2/3 small molecule inhibitor — has entered IND-enabling studies, with its findings selected for a poster presentation at AACR 2025. In addition, the investigational new drug (IND) application for APL-1202 in the treatment of free-living amoebae (FLA) infections was approved by the NMPA in June 2024. In January 2025, the company signed an investigational drug supply agreement under the Expanded Access IND Program with the Centers for Disease Control and Prevention (CDC) in the United States for APL-1202, subject to evaluation by CDC experts, to be used for treating FLA infections. Dr. Kevin Pan, Founder, Chairman and CEO of Asieris Pharmaceuticals, commented, "2024 marks our first full year of commercialization. We delivered strong growth across our marketed products and reached a milestone by breaking even in our commercial operations. Our pipeline is entering a critical sprint toward market launch and is set to power the next wave of performance growth. While reinforcing our commercial capabilities, we're also accelerating clinical programs with a strategic focus on women's health and urological oncology. We're building a robust pipeline of first-in-class and highly-differentiated fast-follow therapies, while actively expanding into global markets to unlock the full value of our assets. With relentless innovation and execution, we are confident that Asieris will continue to make a meaningful difference for patients, deliver solid returns to shareholders, and create lasting value for society." Note: As of the date of this publication, APL-1702 has not been approved for the treatment of cervical high-grade squamous intraepithelial lesions (HSIL). This article is intended to disclose the latest development of these products, not to serve as a promotional advertisement for the products. The relevant information is not intended for patients but is provided solely for the reference of healthcare professionals. If you like to learn more about these diseases, please consult healthcare professionals. SOURCE Asieris WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED