Efficacy and Safety of Dalpiciclib Combined With Endocrine Adjuvant Therapy in Early-stage HR-positive/HER2-negative Breast Cancer: a Multicenter, Prospective Clinical Study

This study aims to evaluate the efficacy and safety of adjuvant endocrine therapy combined with dalpiciclib at different doses and durations in patients with hormone receptor (HR)-positive, HER2-negative early-stage breast cancer.
It is a multicenter, prospective clinical study. All enrolled patients will receive either dalpiciclib 125 mg for 2 years or dalpiciclib 100 mg for 3 years, in combination with standard endocrine therapy.
The primary endpoint is 3-year invasive disease-free survival (iDFS).

Start Date01 Sep 2025

Sponsor / Collaborator

Fujian Cancer Hospital

NCT07037199

/ Not yet recruitingPhase 2IIT

The Efficacy and Safety of SHR-A1811 Sequential Dalpiciclib Combined With Endocrine Therapy in HR+/HER2-Low/Ultra-Low Advanced Breast Cancer

This multicenter, prospective phase II clinical trial evaluates the efficacy and safety of sequential SHR-A1811 followed by dalpiciclib plus endocrine therapy (fulvestrant or aromatase inhibitors) in 45 patients with HR+/HER2-low/ultra-low advanced breast cancer. Enrolled patients will receive SHR-A1811 monotherapy for 6-8 cycles until clinical benefit, then transition to dalpiciclib with endocrine therapy until disease progression or unacceptable toxicity. The primary endpoint is progression-free survival (PFS), with secondary endpoints including objective response rate (ORR), overall survival (OS), and treatment-related adverse events (TRAEs). The study will be conducted at Sun Yat-sen Memorial Hospital and collaborating centers.

Start Date20 Jun 2025

Sponsor / Collaborator

Sun Yat-Sen Memorial Hospital

NCT06810492

/ Not yet recruitingNot ApplicableIIT

A Single-arm Exploratory Study of the Efficacy and Safety of CDK4/6 Inhibitors in Combination with Endocrine Therapy in the Neoadjuvant Treatment of HR+/HER2- Early Breast Cancer

To explore the efficacy and safety of CDK4/6 inhibitors combined with endocrine neoadjuvant therapy for stage II-III HR-positive/HER2-negative breast cancer.
This study adopts a single-arm, open-label design, and plans to include 40 patients with stage II-III HR+/HER2- breast cancer.

Start Date01 Apr 2025

Sponsor / Collaborator

Hubei Cancer Hospital

100 Clinical Results associated with Dalpiciclib Isethionate

100 Translational Medicine associated with Dalpiciclib Isethionate

100 Patents (Medical) associated with Dalpiciclib Isethionate

Literatures (Medical) associated with Dalpiciclib Isethionate

01 Apr 2025·Cancer Communications

A prospective, phase II, neoadjuvant study based on chemotherapy sensitivity in HR+/HER2‐ breast cancer‐FINEST study

Article

Author: Liu, Guang‐Yu ; Li, Jun‐Jie ; Wu, Wen‐Ya ; Liang, Fei ; Wu, Jiong ; Yu, Ke‐Da ; Chen, Li ; Wang, Zhong‐Hua ; Di, Gen‐Hong ; Shao, Zhi‐Ming ; Fan, Lei

Abstract:

Background:

Hormone receptor‐positive (HR+)/humaal growth factor receptor 2‐negative (HER2‐) breast cancer, the most common breast cancer type, has variable prognosis and high recurrence risk. Neoadjuvant therapy is recommended for median‐high risk HR+/HER2‐ patients. This phase II, single‐arm, prospective study aimed to explore appropriate neoadjuvant treatment strategies for HR+/HER2‐ breast cancer patients.

Methods:

Eligible female patients with newly diagnosed, untreated HR+/HER2‐ breast cancer received 2 cycles of nab‐paclitaxel and carboplatin (nabPCb). Magnetic resonance imaging (MRI) was performed to assess tumor responses, and 40% regression of the maximal tumor diameter was deemed chemo‐sensitive. Chemo‐sensitive patients continued nabPCb for 4 more cycles (group A). Chemo‐insensitive patients were randomized to groups B, C, and D at a ratio of 1:3:1 to receive a new chemotherapy for 4 cycles or endocrine‐immune‐based therapy (dalpiciclib, letrozole and adebrelimab, with goserelin if patients were premenopausal) for 4 cycles or to undergo surgery. Peripheral blood and core‐needle biopsy (CNB) samples were collected before treatment, followed by a next‐generation sequencing (NGS) panel detection and similarity network fusion (SNF) typing through digital pathology data. The primary endpoint was the pathological complete response (pCR) rate, and the secondary endpoint was the clinical objective response rate (ORR).

Results:

A total of 121 patients were enrolled (67.8% with stage III disease), with 76, 9, 27, and 9 patients in groups A, B, C and D, respectively. The total pCR rate was 4.1%, and all patients who received pCR were in group A. Group C had a better ORR than Group B (81.5% vs. 66.7%). Exploratory analysis revealed that patients with the SNF4 subtype were the most sensitive to nabPCb (pCR rate of 21.1% vs. 1.8% in group A), whereas patients in group C with the SNF2 subtype were more sensitive to endocrine‐immune‐based therapy (Miller‐Payne grade 4‐5, 45.5% vs. 6.3%).

Conclusions:

Converting to endocrine‐immune‐based therapy improved the ORR, but not the pCR rate in chemo‐insensitive patients. Neoadjuvant chemotherapy and endocrine therapy are not mutually exclusive. The SNF4 subtype of HR+/HER2‐ breast cancer was more chemo‐sensitive, whereas the SNF2 subtype might be more sensitive to immunotherapy.

01 Feb 2025·BREAST

Influence of ethnicity on cyclin-dependent kinase inhibitor efficacy and toxicity: A systematic review and meta-analysis

Review

Author: De Santis, Pierluigi ; Pagliuca, Martina ; Arpino, Grazia ; De Laurentiis, Michelino ; Giuliano, Mario ; De Angelis, Carmine ; Pavone, Giuliana ; Longobardi, Alessandra ; Caputo, Roberta ; Caltavituro, Aldo ; Puglisi, Fabio ; Del Mastro, Lucia ; Tafuro, Margherita ; Buonaiuto, Roberto

BACKGROUND:

The combination of cyclin-dependent kinase 4 and 6 inhibitors (CDK4/6i) with endocrine therapy (ET) is the standard of care for patients with hormone receptor-positive/human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced breast cancer (aBC). While the efficacy and safety profiles of CDK4/6i and ET have been extensively evaluated in phase II and III trials worldwide, it remains unclear whether the response to CDK4/6i and toxicity profile vary among Asian and non-Asian patients. Therefore, we aimed to assess the treatment efficacy of ET with and without CDK4/6i by comparing outcomes in Asian and non-Asian subgroups included in these clinical trials. In addition, we evaluated the toxicity profiles of the treatments by estimating the risk of treatment-related adverse events (AEs).

METHODS:

We conducted a meta-analysis including the most recent randomized trial data systematically searched from PubMed, Embase, Web of Science, Cochrane CENTRAL (from inception to May 31st, 2024) or presented in abstracts or oral presentations at the ESMO, ASCO, and SABCS international congresses. We included studies comparing CDK4/6i (palbociclib, ribociclib, abemaciclib, dalpiciclib) + ET versus placebo + ET. Progression-free survival (PFS) and overall survival (OS), hazard ratios (HR), and 95 % confidence intervals (CI) were extracted for the two subgroups of interest. To evaluate the treatment-related toxicity profiles, we extracted the number of side effects to estimate the risk of treatment-emergent AEs.

RESULTS:

Eleven studies (n = 5129) were included in this meta-analysis. The addition of CDK4/6i to ET consistently improved PFS in both Asian (HR = 0.52, 95 % CI 0.47-0.60; p < 0.001) and non-Asian (HR = 0.58, 95 % CI 0.52-0.64; p < 0.001) groups. Similarly, the combination of CDK4/6i + ET led to an OS improvement in both Asian (HR = 0.75, 95 % CI 0.62-0.91; p = 0.003) and non-Asian (HR = 0.81, 95 % CI 0.73-0.89; p < 0.001) patients. The risk of treatment related toxicity was higher in the CDK4/6i + ET arm in both Asian and non-Asian groups. Interestingly, a numerically higher rate of treatment-related hematological toxicity was observed in Asian patients, although no significant interethnic difference was found in the relative risk of these events.

CONCLUSIONS:

The combination of CDK4/6i and ET significantly improves PFS and OS compared to ET alone in both Asian and non-Asian patients with HR+/HER2-aBC. Although the magnitude of benefit appears to be independent of ethnicity, future clinical trials should devise a standardized method for stratifying patients by ethnicity to more effectively assess potential differences in treatment benefits.

SYSTEMATIC REVIEW REGISTRATION:

PROSPERO registration number: CRD42024543217.

23 Jan 2025·JOURNAL OF MEDICINAL CHEMISTRY

Elucidating Binding Selectivity in Cyclin-Dependent Kinases 4, 6, and 9: Development of Highly Potent and Selective CDK4/9 Inhibitors

Article

Author: Xing, Yajie ; Cao, Qixiong ; Chen, Jiean ; Wang, Rui ; Yang, Qianqian ; Pan, Shuqiong ; Feng, Meixi ; He, Zhipeng ; Huang, Yong ; Jiang, Chenran ; Lian, Chenshan ; Kang, Wei ; Yang, Jinglei ; Liu, Zhihong ; Wu, Yun-Dong ; Yin, Feng ; Ye, Yuxin ; Zhao, Juan ; Song, Chunli

CDK4/6 inhibitors are effective in treating HR⁺/HER2^- breast cancer but face limitations due to therapeutic resistance and hematological toxicity, particularly from strong CDK6 inhibition. To address these challenges, designing selective inhibitors targeting specific cyclin-dependent kinases (CDK) members could offer clinical advantages and broaden CDK inhibitor indications. However, the highly conserved binding pockets of CDKs complicate selective targeting. This study leverages in silico modeling and structural analysis of cocrystal data to identify subtle differences in key CDK binding pockets. Notably, a sequence difference in the αD-helix motif between CDK4 and CDK6 provides a targetable "sweet spot" for selectivity. By incorporating a 1,4-trans-cyclohexanediamine side chain, we designed molecules that favor interactions with CDK4 over CDK6 and explored potential dual CDK4/9 inhibition. This approach yielded a lead compound with distinct in vitro selectivity and promising in vivo pharmacokinetics, offering valuable insights for the development of selective next-generation CDK inhibitors.

News (Medical) associated with Dalpiciclib Isethionate

05 Jun 2025

·www.prnewswire.com

Hengrui Pharma Showcases Global Impact at the 2025 ASCO: 72 Study Results Highlight Chinese Cancer Innovation

SHANGHAI, June 5, 2025 /PRNewswire/ -- The 2025 ASCO Annual Meeting successfully concluded in Chicago on June 3 (local time). Hengrui Pharma delivered a strong international presence, featuring 15 innovative drugs and 72 research outcomes. These included 4 oral presentations, 5 rapid oral presentations, 27 poster presentations, and 36 online publications. Multiple groundbreaking research advances has elicited widespread discussion among global experts. In the field of breast cancer, results from 19 studies evaluating the company's innovative drugs—pyrotinib, dalpiciclib, camrelizumab, apatinib, adebrelimab, Trastuzumab rezetecan (SHR-A1811), and SHR-2017, either in combination with each other or with chemotherapies, were presented at ASCO 2025. Notably, 7 studies involving pyrotinib and 6 studies involving dalpiciclib were selected, with both agents consistently demonstrating promising efficacy, reinforcing their established roles in breast cancer treatment. Furthermore, studies evaluating SHR-A1811 and adebrelimab were selected for rapid oral presentations, attracting considerable attention from the industry. In the field of gastrointestinal cancers, drugs such as camrelizumab, apatinib, adebrelimab, and SHR-8068 were featured in a total of 30 accepted studies. Notably, camrelizumab was included in 21 of these studies, demonstrating its broad therapeutic profile and potential while reinforcing its position as a key focus at ASCO. This further solidifies the achievements of China-developed PD-1 inhibitors on the global stage. Additionally, adebrelimab, which has achieved significant breakthroughs in lung cancer in recent years, is actively expanding into new indications. At this year's ASCO, five related studies exploring adebrelimab's efficacy in indications such as hepatocellular carcinoma (HCC), cholangiocarcinoma (CCA) , and pancreatic cancer were presented. The ongoing emergence of cutting-edge research on both established and emerging agents holds promise for improving clinical outcomes for patients with gastrointestinal tumors. Across a wide range of disease areas—including lung cancer, gynecologic cancers, lymphoma, bladder cancer, head and neck cancer, melanoma, sarcoma, nasopharyngeal carcinoma, chordoma, salivary gland cancer, thymic cancer, desmoid tumors, and salivary duct carcinoma—Hengrui Pharma's innovative oncology portfolio (camrelizumab, apatinib, adebrelimab, pyrotinib, dalpiciclib, fluzoparib, famitinib, SHR-A1811, SHR-1501, SHR-1701, SHR-1826, SHR-A1912, and SHR-A2102) was featured in 22 research presentations at ASCO 2025. These comprised 4 oral presentations, 2 rapid oral presentations, 12 poster presentations, and 4 online publications, collectively demonstrating the company's robust R&D capabilities. Additionally, one online publication highlighted ondansetron oral soluble film, underscoring its favorable efficacy in preventing and treating chemotherapy-induced nausea and vomiting (CINV). For 15 consecutive years, Hengrui Pharma has consistently presented its cutting-edge research at the ASCO Annual Meeting, highlighting the company's global leadership in oncology drug research and development while showcasing China's robust pharmaceutical innovation capabilities to the international academic community. The inclusion of 70 Hengrui-sponsored studies at this year's meeting reflects the strong foundation laid by the company's portfolio of 23 marketed innovative drugs and a robust pipeline of over 90 candidates currently in development. Looking ahead, Hengrui will remain committed to its patient-centric approach, striving to develop advanced therapeutics that support the "Healthy China" initiative and enhance clinical outcomes for patients globally. SOURCE Hengrui Pharma WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

ASCOClinical ResultCSCO

15 Oct 2024

·www.prnewswire.com

Metastatic Castration-Sensitive Prostate Cancer Clinical Trial Pipeline Insights Featuring 35+ Companies | DelveInsight

Metastatic castration-sensitive prostate cancer (mCSPC), also known as metastatic hormone-sensitive prostate cancer (mHSPC), refers to prostate cancer that has spread beyond the prostate but still responds to therapies that lower testosterone (castration) with an aging population, the incidence of prostate cancer is rising, leading to an increased demand for advanced therapies to treat metastatic forms of the disease. LAS VEGAS, Oct. 15, 2024 /PRNewswire/ -- DelveInsight's ' Metastatic Castration-Sensitive Prostate Cancer Pipeline Insight 2024 ' report provides comprehensive global coverage of pipeline mCSPC therapies in various stages of clinical development, major pharmaceutical companies are working to advance the pipeline space and future growth potential of the mCSPC pipeline domain. Key Takeaways from the Metastatic Castration-Sensitive Prostate Cancer Pipeline Report DelveInsight's mCSPC pipeline report depicts a robust space with 35+ active players working to develop 40+ pipeline therapies for mCSPC treatment. Key mCSPC companies such as Tavanta Therapeutics, AstraZeneca, Regeneron Pharmaceuticals, Astellas Pharma, Propella Therapeutics, POINT Biopharma, Amgen, Janssen Research & Development, LLC, Bayer, Beigene, Amgen, Merck Sharp & Dohme LLC, Jiangsu HengRui Medicine Co., Ltd., Suzhou Kintor Pharmaceutical Inc, Astellas Pharma, and others are evaluating new mCSPC drugs to improve the treatment landscape. Promising mCSPC pipeline therapies such as TAVT-45 (abiraterone acetate), Saruparib (AZD5305), Capivasertib, REGN2810, Abiraterone decanote + dexamethasone or prednisone (PRL-02/ASP5541), [Ac-225]-PSMA-62, Xaluritamig, Apalutamide, Darolutamide, Luteinizing Hormone Releasing Hormone, Pembrolizumab, Dalpiciclib isethionate, GT0918, PRL-02, and others are under different phases of mCSPC clinical trials. In October 2024, Apalutamide (Erleada) was found to provide a significant improvement in overall survival (OS) at 24 months compared with enzalutamide (Xtandi) in the treatment of androgen receptor pathway inhibitor (ARPI)-naïve patients with metastatic castration-sensitive prostate cancer (mCSPC). In April 2024, Saruparib (AZD5305) demonstrated encouraging efficacy, favorable safety, a wide therapeutic index, and improved pharmacokinetic properties compared with currently approved PARP inhibitors in patients with advanced solid tumors harboring BRCA1/2, PALB2, or RAD51C/D mutations, according to findings from the Phase I/IIa PETRA study. In February 2024, Capivasertib combined with docetaxel to enhance anti-tumour activity through inhibition of AKT-mediated survival mechanisms in prostate cancer. Capivasertib can enhance anti-tumour effects of docetaxel by targeting residual docetaxel-persister cells, independent of PTEN status, to induce apoptosis and DNA damage in part through GSK3β. In January 2023, Tavanta Therapeutics announced positive top-line results from its pivotal, global Phase III clinical trial, evaluating the safety and efficacy of TAVT-45 (abiraterone acetate). The trial met its primary objective of establishing therapeutic equivalence of TAVT-45 to Zytiga® in patients with metastatic castrate-resistant prostate cancer (mCRPC) and metastatic high-risk castrate-sensitive prostate cancer (mCSPC), in addition to demonstrating a comparable safety profile. Request a sample and discover the recent advances in mCSPC treatment drugs @ Metastatic Castration-Sensitive Prostate Cancer Pipeline Report The mCSPC pipeline report provides detailed profiles of pipeline assets, a comparative analysis of clinical and non-clinical stage mCSPC drugs, inactive and dormant assets, a comprehensive assessment of driving and restraining factors, and an assessment of opportunities and risks in the mCSPC clinical trial landscape. Metastatic Castration-Sensitive Prostate Cancer Overview Metastatic castration-sensitive prostate cancer (mCSPC) is an advanced form of prostate cancer in which the cancer cells have spread beyond the prostate to other parts of the body, such as bones or lymph nodes, but remain responsive to hormone therapy. This means that reducing testosterone levels can still effectively slow the growth of cancer cells. mCSPC often arises when prostate cancer is initially diagnosed or when early-stage prostate cancer recurs after treatment. It is distinct from castration-resistant prostate cancer (CRPC), where the cancer continues to progress despite low testosterone levels. The causes of mCSPC primarily involve the spread of prostate cancer cells beyond the local prostate region, a process called metastasis. Although the exact mechanisms are complex, certain risk factors increase the likelihood of developing prostate cancer and its progression to metastatic disease. These risk factors include advanced age, a family history of prostate cancer, genetic mutations such as BRCA1/BRCA2, and race. Symptoms of mCSPC can include bone pain, urinary issues, fatigue, weight loss, and general malaise, especially if the cancer has spread to bones or lymph nodes. However, in many cases, early stages of metastasis may be asymptomatic, making regular screening essential for those at risk. Diagnosis of mCSPC typically involves a combination of blood tests, such as measuring prostate-specific antigen (PSA) levels, imaging studies, and biopsy to confirm the presence of cancer cells. Treatment for mCSPC revolves around androgen deprivation therapy to lower testosterone levels, often combined with other agents like chemotherapy (e.g., docetaxel) or second-generation androgen receptor inhibitors (e.g., abiraterone or enzalutamide). In recent years, clinical trials have shown the benefit of combining ADT with novel therapies to improve survival rates and manage symptoms, with personalized treatment approaches based on genetic testing becoming more common. Find out more about mCSPC treatment drugs @ Drugs for Metastatic Castration-Sensitive Prostate Cancer Treatment A snapshot of the mCSPC Pipeline Drugs mentioned in the report: Learn more about the emerging mCSPC pipeline therapies @ Metastatic Castration-Sensitive Prostate Cancer Clinical Trials Metastatic Castration-Sensitive Prostate Cancer Therapeutics Assessment The mCSPC pipeline report proffers an integral view of the mCSPC emerging novel therapies segmented by stage, product type, molecule type, mechanism of action, and route of administration. Scope of the Metastatic Castration-Sensitive Prostate Cancer Pipeline Report Coverage: Global Therapeutic Assessment By Product Type: Mono, Combination, Mono/Combination Therapeutic Assessment By Clinical Stages: Discovery, Pre-clinical, Phase I, Phase II, Phase III Therapeutics Assessment By Route of Administration: Oral, Intravenous, Subcutaneous Therapeutics Assessment By Molecule Type: Small molecule, Cell therapy, Peptides, Polymer, Small molecule, Gene therapy Therapeutics Assessment By Mechanism of Action: Steroidal inhibitor of CYP17A1, PARP1 inhibitor, Proto-oncogene protein c-akt inhibitors, CYP17 lyase inhibitor, Antibody-dependent cell cytotoxicity, Immunostimulants, T lymphocyte stimulants, Ionizing radiation emitters. Key Metastatic Castration-Sensitive Prostate Cancer Companies: Tavanta Therapeutics, AstraZeneca, Regeneron Pharmaceuticals, Astellas Pharma, Propella Therapeutics, POINT Biopharma, Amgen, Janssen Research & Development, LLC, Bayer, Beigene, Amgen, Merck Sharp & Dohme LLC, Jiangsu HengRui Medicine Co., Ltd., Suzhou Kintor Pharmaceutical Inc, Astellas Pharma, and others. Key Metastatic Castration-Sensitive Prostate Cancer Pipeline Therapies: TAVT-45 (abiraterone acetate), Saruparib (AZD5305), Capivasertib, REGN2810, Abiraterone decanote + dexamethasone or prednisone (PRL-02/ASP5541), [Ac-225]-PSMA-62, Xaluritamig, Apalutamide, Darolutamide, Luteinizing Hormone Releasing Hormone, Pembrolizumab, Dalpiciclib isethionate, GT0918, PRL-02, and others. Dive deep into rich insights for new drugs for mCSPC treatment, visit @ Metastatic Castration-Sensitive Prostate Cancer Drugs Table of Contents For further information on the mCSPC Cancer pipeline therapeutics, reach out @ Metastatic Castration-Sensitive Prostate Cancer Treatment Drugs Related Reports Metastatic Castration-Sensitive Prostate Cancer Market Metastatic Castration-Sensitive Prostate Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and key mCSPC companies including Myovant Sciences, Pfizer, Bayer, Orion, Novartis, AstraZeneca, Pfizer, Janssen, Merck, Eli Lilly, among others. Metastatic Prostate Cancer Market Metastatic Prostate Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and 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 – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and key mCRPC companies including 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, among others. Metastatic Castration-Resistant Prostate Cancer Pipeline Metastatic Castration-Resistant Prostate Cancer Pipeline Insight – 2024 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key mCRPC companies, including 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, 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] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Clinical Result

17 Nov 2023

·synapse.patsnap.com

What are CDK4 inhibitors and how do you quickly get the latest development progress?

CDK4, or cyclin-dependent kinase 4, is a crucial protein involved in cell cycle regulation in the human body. It plays a significant role in controlling the progression of cells from the G1 phase to the S phase, where DNA replication occurs. CDK4 forms a complex with cyclin D, which activates its kinase activity. This activation leads to the phosphorylation of key proteins involved in cell cycle progression, allowing cells to transition from the resting phase to the active phase of cell division. Dysregulation of CDK4 activity has been associated with various diseases, including cancer, making it an important target for pharmaceutical interventions. In ER+ breast cancer, estrogen signaling increases the activity of the ER- cell cycle protein D1-CDK4/6 pathway, driving cells from the G1 phase into the S phase, ultimately leading to uncontrolled cell proliferation. CDK4/6 inhibitors can inhibit the formation of a complex between CDK4/6 and cell cycle protein D, block ATP binding, thus interrupting upstream growth signals and preventing the transition from G1 phase to S phase. The CDK inhibitors currently approved by the FDA are all CDK4/6 inhibitors: Pfizer's Palbociclib (PD-0332991, 21), Novartis's Ribociclib (LEE011, 22), Eli Lilly's Abemaciclib (LY-2835219,23) and G1 Therapeutics' Trilaciclib (G1T28,24). The ATP binding domains of CDK4 and CDK6 exhibit high structural similarity, with differences only between Glu144 (CDK4) and Gln149 (CDK6). These four inhibitors are all ATP-competitive inhibitors, capable of binding with the kinase's ATP binding domain. The analysis of the target CDK4 reveals a competitive landscape with several companies actively involved in the research and development of drugs. Novartis AG and Pfizer Inc. are leading the way with drugs in advanced stages of development. The indications for the target CDK4 primarily focus on breast cancer, with several drugs approved for hormone receptor-positive HER2-negative breast cancer. Small molecule drugs are progressing rapidly, indicating intense competition around innovative drugs. China and the United States are the frontrunners in terms of development, with China showing significant progress. Overall, the target CDK4 presents a promising future in the pharmaceutical industry. How do they work?CDK4 inhibitors are a type of drug that specifically target and inhibit the activity of cyclin-dependent kinase 4 (CDK4). CDK4 is an enzyme that plays a crucial role in regulating the cell cycle, specifically in the transition from the G1 phase to the S phase. By inhibiting CDK4, these inhibitors help to prevent the uncontrolled cell growth and proliferation that is characteristic of cancer. From a biomedical perspective, CDK4 inhibitors are a promising class of drugs in the field of oncology. They have shown potential in the treatment of various types of cancer, including breast cancer, melanoma, and glioblastoma. By blocking the activity of CDK4, these inhibitors can halt the cell cycle progression and induce cell cycle arrest, leading to the inhibition of tumor growth. CDK4 inhibitors are often used in combination with other cancer therapies, such as chemotherapy or targeted therapies, to enhance their effectiveness. They can also be used as single agents in certain cases. These inhibitors are typically administered orally in the form of pills or tablets. It's important to note that CDK4 inhibitors are prescription drugs and should only be used under the supervision of a qualified healthcare professional. They may have side effects, such as nausea, fatigue, and low blood cell counts, which need to be monitored during treatment. Additionally, individual response to CDK4 inhibitors may vary, and not all patients may benefit from this type of therapy. List of CDK4 InhibitorsThe currently marketed CDK4 inhibitors include: Trilaciclib DihydrochlorideDalpiciclib IsethionateAbemaciclibLetrozole/Ribociclib SuccinateRibociclib SuccinatePalbociclibBirociclibLerociclibBEBT-209BPI-16350For more information, please click on the image below. What are CDK4 inhibitors used for?CDK4 inhibitors primarily focus on breast cancer, with several drugs approved for hormone receptor-positive HER2-negative breast cancer.For more information, please click on the image below to log in and search. How to obtain the latest development progress of CDK4 inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of CDK4 inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Dalpiciclib Isethionate

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hormone receptor positive HER2 negative breast cancer	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	31 Dec 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Castration-sensitive prostate cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	19 Oct 2023
HER2-negative breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	30 Apr 2021
Hormone receptor positive breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	30 Apr 2021
Node-positive breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	30 Apr 2021
Advanced breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	13 Jun 2019
HR Positive/HER2 Negative/Node positive breast cancer	Phase 3	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	13 Jun 2019
Metastatic castration-resistant prostate cancer	Phase 2	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	31 Jul 2024
ER-positive/HER2-negative Breast Cancer	Phase 2	China	Shandong Suncadia Medicine Co., Ltd.	20 Dec 2023
Ewing Sarcoma	Phase 2	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Jul 2023
Metastatic Soft Tissue Sarcoma	Phase 2	China	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Jul 2023

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05586841 (ASCO2025) Manual	Phase 1	Hormone receptor positive HER2 negative breast cancer HER2 Negative \| HR Positive	22	dalpiciclib + chidamide	wbkvcfhkgq(nmiptojedm) = the MTD was established as Group C (dalpiciclib 100 mg/d, chidamide 25 mg BIW). scrdjoedul (oiksmpvsma )	Positive	30 May 2025
				dalpicicldalpiciclibchidamide (Group C: dalpiciclib 100 mg/d, chidamide 25 mg BIW)
NCT06495515 (ASCO2025)	Phase 2	HR Positive/HER2 Negative/Node positive breast cancer First line HR+ \| HER2-negative	26	Dalpiciclib plus Toremifene	hvqeprjyxr(rqdbralkyv) = ehegpsveap idchcepfmv (vbiuifzcgo ) View more	Positive	30 May 2025
NCT05806671 (Bayesian optimal phase Ⅱ trial, ASCO2025)	Phase 2	HR-positive/HER2-low Breast Carcinoma	30	Dalpiciclib plus Fulvestrant and Pyrotinib	ujnxxsvpjr(jujjlzvqlu) = ydbgigtglh ucdjfdchre (busszbzdtk ) View more	Positive	30 May 2025
				Abemaciclib	jtatcnknbr(flirrgqypa) = luombpgiht fnaiotrqmz (bfciejxydk, 1.1 - 5.1)
NCT04842617 (DAWNA-A, ASCO2025)	Phase 3	Early Stage Breast Carcinoma Adjuvant HR+ \| HER2-	5,274	Dalpiciclib (Dalp) + Endocrine Therapy (ET)	nwmiiaonsc(ndbptcmnli): HR = 0.56 (95% CI, 0.43 - 0.71)	Positive	30 May 2025
				Placebo + Endocrine Therapy (ET)
NCT05640778 (DANCER, ASCO2025)	Phase 2	HER2-negative breast cancer Neoadjuvant ctDNA clearance \| Olink proteomic analyses \| somatic variation profiling ... View more	30	dalpiciclib (Good Responders (GR))	fkvbzcerkj(gynuzwalrc) = significant shift in copy number pattern after treatment at S htfjkajpxn (ypqnqjvvnp )	Positive	30 May 2025
				dalpiciclib (Moderate Responders (MR))
CTR20210652 (DAWNA-A \| SHR6390-III-303, NEWS) Manual	Phase 3	Hormone receptor positive HER2 negative breast cancer HER2 Negative \| HR Positive	5,000	羟乙磺酸达尔西利+内分泌治疗	anulgtjeib(eurvywhubs) = 达尔西利联合内分泌治疗，较安慰剂联合内分泌治疗，可显著降低患者复发风险，提高患者无侵袭性疾病生存期 mlamzvvvfo (idvqrqcvdr ) Met	Positive	23 Feb 2025
				安慰剂+内分泌治疗
NCT05512780 (DARLING 01, Pubmed \| Breast Cancer Res) Manual	Phase 2	Hormone receptor positive HER2 negative breast cancer Neoadjuvant HER2 Negative \| HR Positive	29	Dalpiciclib + Letrozole	ajhotcubsg(eiinskcozh) = sccpibyvxx luhwephqfn (ynmvadsyqq ) View more	Positive	13 Feb 2025
NCT03966898 (DAWNA-2, SABCS2024) Manual	Phase 3	Hormone receptor positive HER2 negative breast cancer First line HR Positive \| HER2 Negative	456	Dalpiciclib + Letrozole/Anastrozole	duicioycny(wleinypghp) = tvtnoefeal cvcklgciot (cuvggagebg, 29.6 - 39.0) View more	Positive	12 Dec 2024
				Placebo + Letrozole/Anastrozole	duicioycny(wleinypghp) = jlrsjlqbgh cvcklgciot (cuvggagebg, 16.5 - 22.5) View more
NCT05431504 (SABCS2024 \| NEWS) Manual	Phase 2	Hormone receptor positive HER2 negative breast cancer HR Positive \| HER2 Negative	53	Dalpiciclib plus ET	qyooknouvz(joxthmnokc) = agyypuyadb jjaksllrxj (gvyjwggrni, 7.59 - NE) View more	Positive	26 Nov 2024
				Chemotherapy (external control group)	qyooknouvz(joxthmnokc) = rbyexaawhx jjaksllrxj (gvyjwggrni, 2.92 - 5.91) View more
NCT06009627 (ESMO2024) Manual	Phase 2	Premenopausal breast cancer Neoadjuvant HER2 Negative \| HR Positive	32	Dalpiciclib, Exemestane, and Goserelin	myeuyhytxt(iknxkiqulp) = qtxatxyaxt xiyeyvtpjd (wxzbrhrynq )	Positive	16 Sep 2024
				TAC (docetaxel, doxorubicin, and cyclophosphamide)	myeuyhytxt(iknxkiqulp) = fvmediptvn xiyeyvtpjd (wxzbrhrynq )

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