Last update 10 Nov 2024
Tagtociclib
Last update 10 Nov 2024
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms PF 07104091, PF-07104091, PF07104091 |
Target |
Mechanism CDK2 inhibitors(Cyclin-dependent kinase 2 inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication- |
Originator Organization |
Active Organization |
Inactive Organization- |
Drug Highest PhasePhase 1/2 |
First Approval Date- |
Regulation- |
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Structure
Molecular FormulaC19H28N6O4 |
InChIKeyMTNBRBDFNSGQKB-GXTWGEPZSA-N |
CAS Registry2460249-19-6 |
Related
6
Clinical Trials associated with Tagtociclib一项在晚期实体瘤受试者中评价 PF-07220060 联合 PF-07104091 和内分泌治疗的安全性、耐受性、药代动力学、药效学和抗肿瘤活性的 IB/II 期、开放性、多中心、剂量递增和剂量扩展研究
[Translation] A Phase IB/II, open-label, multicenter, dose-escalation and dose-expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 and endocrine therapy in subjects with advanced solid tumors
第 1部分：
评估递增剂量的 PF-07220060 和 PF-07104091 联合治疗在晚期实体瘤受试者中的安全性和耐受性，以估计 MTD 并选择 RDE。
第2部分：
评估按选定的 RDE 在 HR 阳性 HER2 阴性晚期或 mBC 受试者中进行 PF-07220060、PF-07104091 和 ET（第 2A 和 2B 部分为氟维司群；第 2C 部分为来曲唑）联合治疗的安全性和耐受性。
[Translation]
Part 1:
To evaluate the safety and tolerability of escalating doses of PF-07220060 and PF-07104091 combination therapy in subjects with advanced solid tumors to estimate the MTD and select an RDE.
Part 2:
To evaluate the safety and tolerability of PF-07220060, PF-07104091, and ET (fulvestrant in Parts 2A and 2B; letrozole in Part 2C) combination therapy at the selected RDE in subjects with HR-positive HER2-negative advanced or mBC.
Start Date19 Jul 2023 |
Sponsor / Collaborator  Pfizer Inc. [+1] |
一项在晚期实体瘤受试者中评价 PF-07220060 联合 PF-07104091 和内分泌治疗的安全性、耐受性、药代动力学、药效学和抗肿瘤活性的 IB/II 期、开放性、多中心、剂量递增和剂量扩展研究
[Translation] A Phase IB/II, open-label, multicenter, dose-escalation and dose-expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 and endocrine therapy in subjects with advanced solid tumors
第 1部分：
评估递增剂量的 PF-07220060 和 PF-07104091 联合治疗在晚期实体瘤受试者中的安全性和耐受性，以估计 MTD 并选择 RDE。
第2部分：
评估按选定的 RDE 在 HR 阳性 HER2 阴性晚期或 mBC 受试者中进行 PF-07220060、PF-07104091 和 ET（第 2A 和 2B 部分为氟维司群；第 2C 部分为来曲唑）联合治疗的安全性和耐受性。
[Translation]
Part 1:
To evaluate the safety and tolerability of escalating doses of PF-07220060 and PF-07104091 combination therapy in subjects with advanced solid tumors to estimate the MTD and select an RDE.
Part 2:
To evaluate the safety and tolerability of PF-07220060, PF-07104091, and ET (fulvestrant in Parts 2A and 2B; letrozole in Part 2C) combination therapy at the selected RDE in subjects with HR-positive HER2-negative advanced or mBC.
Start Date19 Jul 2023 |
Sponsor / Collaborator Pfizer Inc. [+1] |
一项评估 PF-07104091 单药治疗和联合治疗的安全性、耐受性、药代动力学、药效学和抗肿瘤活性的 I/IIA 期、剂量递增、探索和扩展研究
[Translation] A Phase I/IIA, dose-escalation, exploratory, and expansion study evaluating the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07104091 as monotherapy and in combination
1A 部分：在以下受试者中评估递增剂量的PF-07104091安全性和耐受性以及估计PF-07104091单药的MTD和/或选择RDE：晚期或转移性SCLC；晚期铂类耐药上皮性卵巢癌/输卵管癌/原发性腹膜癌；局部复发性/晚期或转移性TNBC；HR阳性HER2阴性晚期或mBC；晚期或转移性NSCLC。1B、1C 和1D 部分：评估PF-07104091联合CDK4/6抑制剂和内分泌疗法或仅联合内分泌疗法在HR阳性HER2阴性晚期或mBC 患者中的安全性、耐受性，并确定MTD和/或选择RDE。第2 部分：评估PF-07104091在以下方面的初步抗肿瘤活性并确认其安全性和耐受性：作为单药（不高于1A中MTD/RDE的剂量）治疗患有晚期或转移性SCLC的受试者以及患有晚期铂类耐药上皮性卵巢癌/输卵管癌/原发性腹膜癌的受试者。作为联合疗法（PF-07104091+哌柏西利和内分泌疗法或PF-07104091+氟维司群）治疗CDK4/6经治或未治的HR阳性HER2阴性晚期或mBC受试者。中国队列：分析中国人群的PK特征，评估PF-07104091单药治疗的安全性和耐受性。
[Translation]
Part 1A: To evaluate the safety and tolerability of PF-07104091 at escalating doses and estimate the MTD and/or select RDE of PF-07104091 alone in the following subjects: advanced or metastatic SCLC; advanced platinum-resistant epithelial ovarian/fallopian tube/primary peritoneal cancer; locally recurrent/advanced or metastatic TNBC; HR-positive HER2-negative advanced or mBC; advanced or metastatic NSCLC. Parts 1B, 1C, and 1D: To evaluate the safety, tolerability, and determine the MTD and/or select RDE of PF-07104091 in combination with CDK4/6 inhibitors and endocrine therapy or endocrine therapy alone in patients with HR-positive HER2-negative advanced or mBC. Part 2: Evaluate the preliminary anti-tumor activity of PF-07104091 and confirm its safety and tolerability in the following aspects: As a single agent (no higher than the MTD/RDE in 1A) for the treatment of subjects with advanced or metastatic SCLC and subjects with advanced platinum-resistant epithelial ovarian/fallopian tube/primary peritoneal cancer. As a combination therapy (PF-07104091 + palbociclib and endocrine therapy or PF-07104091 + fulvestrant) for the treatment of CDK4/6-pretreated or untreated HR-positive HER2-negative advanced or mBC subjects. Chinese cohort: Analyze the PK characteristics of the Chinese population and evaluate the safety and tolerability of PF-07104091 monotherapy.
Start Date16 Nov 2022 |
Sponsor / Collaborator Pfizer Inc. [+1] |
100 Clinical Results associated with Tagtociclib
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100 Translational Medicine associated with Tagtociclib
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100 Patents (Medical) associated with Tagtociclib
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4
News (Medical) associated with Tagtociclib11 Oct 2024
On September 30, Genentech, a division of Roche, entered into a major agreement with Rueger, with Genentech successfully acquiring Rueger's portfolio of next-generation CDK inhibitors for $850 million in upfront cash and other potential milestone payments. This transaction not only refreshes the down payment record for the foreign authorization of domestic molecules, but also marks a new milestone in the cooperation between the two sides. The previous record was held by Benefi Tianheng's agreement with BMS for the BL-B01D1 molecule, which was valued at $800 million.
It is worth noting that the transaction between Benefi Tianhengand BMS only involves a single molecule BL-B01D1, which is already in the late clinical stage, and both parties share the subsequent overseas clinical costs. The collaboration with Genentech builds on a broader portfolio of next-generation CDK inhibitors, which is expected to include the Phase I CDK2/4/6 inhibitor RGT-419B and the preclinical CDK2 inhibitor QR-6401. Under the terms of the agreement, Genentech will be responsible for the global clinical development, manufacturing and commercialization of these products after the end of the existing Phase 1 clinical phase.
Recently, the field of CDK inhibitors has become a hot spot pursued by many companies. In addition to Genentech, Beigene also announced the introduction of ETX-197, a CDK2 inhibitor from Onsun Pharma, at the end of November last year. Although the amount of the upfront payment was not disclosed, taking into account potential future milestone payments and sales sharing, the total value of the deal is up to $1.33 billion.
With some generic CDK4/6 inhibitors entering the market in bulk, some investors are questioning whether the competitive landscape on the CDK inhibitor circuit has reached saturation. However, leading companies such as Roche and Beigene are still actively developing next-generation CDK inhibitors, which has a profound scientific and commercial logic behind it.
CDKs (cyclin-dependent kinases), as an important member of the serine/threonine protein kinase family, play a crucial role in cell cycle regulation. CDK family targets are mainly divided into two categories: one is involved in cell cycle regulation and related mitosis, such as CDK1, 2, 4, 6; The other group is mainly involved in transcriptional regulation and phosphorylation of RNA polymerase II, such as CDK7, 8, 9, 11. Among them, CDK4/6 and CDK2 have attracted much attention due to their important roles in the development of tumors.
CDK4/6 is a key condition protein in the human cell division and proliferation cycle, which can trigger the cell cycle transition from the growth phase (G1 phase) to the DNA replication phase (S phase). In many cancer cells, CDK4/6 is overexpressed, which promotes the disorderly proliferation of cancer cells through over-phosphorylation and inhibition of Rb protein. Therefore, CDK4/6 inhibitors can inhibit the proliferation of tumor cells by blocking the cell growth cycle in the G1 phase. CDK2 plays a key role in the early phase of DNA synthesis (G1 phase) and the phase of DNA synthesis (S phase) of the cell cycle, and its overexpression is closely related to the abnormal regulation of the cell cycle and the excessive proliferation of cancer cells.
From a market perspective, breast cancer, as the world's largest malignant tumor (accounting for about 24.5% of all malignant tumors), provides a broad application space for CDK inhibitors. In particular, the large population of HR+/HER2- advanced breast cancer patients (about 60%-70%) makes endocrine therapy combined with CDK4/6 inhibitors a first-line treatment in this area. This also explains why CDK4/6 inhibitors can occupy an important position in the treatment of breast cancer and create a large drug market size.
Despite the proliferation of blockbuster drugs in recent years, existing and older CDK4/6 inhibitors inevitably have several shortcomings, the most significant of which are drug toxicity and resistance.
First, in terms of toxicity, hematotoxicity is the most common side effect of CDK4/6 inhibitors. These inhibitors inhibit cell proliferation by blocking the cell cycle, thus killing rapidly dividing cells, but this mechanism also leads to myelosuppression, which reduces blood cell production. Specifically, neutropenia, leukopenia, anemia, and thrombocytopenia are the most common hematological toxic side effects of commercialized CDK4/6 inhibitors. In addition, CDK4/6 inhibitors may also cause gastrointestinal adverse reactions, which should not be ignored.
Second, in terms of drug resistance, although CDK4/6 inhibitors have achieved remarkable results in improving disease control in HR+/ HER2-breast cancer patients, 15-20% of patients still develop primary resistance to the drug at the beginning of treatment, while 30-40% of patients develop resistance gradually over the course of treatment. The mechanisms of drug resistance are complex and diverse, including but not limited to ESR1 gene mutation, upregulation of PI3K/AKT/mTOR signaling pathway, and BRCA2 gene mutation.
In view of the influx of generic drugs of the older generation of CDK4/6 inhibitors and the urgent need to solve the existing toxicity and drug resistance problems, the new generation of CDK inhibitors ushered in more development opportunities. The RRT-419B that Roche is concerned about is a new generation of CDK2/4/6 small molecule inhibitor developed by Rueger Pharmaceutical. The drug is not commercially available worldwide, and its kinase activity profile has been optimized to target "better" safety and resistance CDK inhibitors from the outset.
Regal's RRT-419B shows unique ingenuity in both design ideas and drug mechanisms, and has achieved preliminary validation of ideas in existing breast cancer clinical data. Unlike existing commercialized CDK inhibitors, which mainly inhibit subtypes 4 and 6, RGT-419B aims to reduce the occurrence of resistance to existing CDK4/6 inhibitors by increasing the inhibition of CDK2 subtypes, thereby achieving long-term efficacy.
When CDK4/6 activity is inhibited, expansion of Cyclin E and activation of the oncogene MYC lead to up-regulation of MYC and activation of CDK2. CDK2-CyclinE, as a compensatory pathway, phosphorylates Rb, thereby releasing E2F transcription factors and promoting tumor cell proliferation. This process is the key to the development of acquired resistance to CDK4/6 inhibitors. Preliminary data from overseas studies such as Pfizer's CDK2 inhibitor PF-07104091 also revealed an association between CDK2 activation and acquired resistance to CDK4/6 inhibitors.
In December 2023, Rueger presented the latest clinical data for RGT-419B at the SABCS Conference. The drug performed well in a Phase 1a clinical trial of monotherapy in 12 patients with HR+/ HER2-metastatic breast cancer receiving CDK4/6is and ET progression: three patients achieved partial response (PR) and continued treatment; Six patients received RGT-419B for more than 24 weeks; The drug was safe and well tolerated, no dose-limiting toxicity occurred, and no patient stopped treatment due to adverse events.
Given the huge potential of next-generation CDK inhibitors in second-line breast cancer monotherapy, and the successful performance of commonly used second-line endocrine drugs such as fluvestrant in the market (such as the peak sales of $1.028 billion for fluvestrant in 2018), the global market for next-generation CDK inhibitors is expected to reach at least $2-3 billion. That is one of the reasons Roche is willing to bet so heavily.
Faced with such a broad market prospect, many domestic pharmaceutical companies have also devoted themselves to the research and development of a new generation of CDK2/4/6 inhibitors or CDK2 inhibitors. One kind of large pharmaceutical companies further expand the development of CDK2 inhibitors on the basis of CDK4/6 inhibitor layout, such as Hengrui Pharmaceutical and First Sound Pharmaceutical; The other category is the first to enter the CDK inhibitor track of Biotech or big pharmaceutical companies such as Ruge Pharmaceutical, Stone pharmaceutical Group and Homology Kang Pharmaceutical. These companies are advancing the CDK inhibitor field and competing for future market share through continuous research and development and innovation.
Although most of the CDK2/4/6 inhibitors that have entered the clinical stage in China are still in the early clinical stage, and most of them have not yet been validated by clinical data, it can be observed from the transaction cases of Regal Medicine and Beigene that these two authorized molecules have been deeply optimized by AI technology.
From the information that has been made public, the AI pharmaceutical platform has played a key driving role in Genentech/Regal Pharma's RGT-419B and Beigene/Angsen Pharma's ETX-197 project. It is worth noting that the high degree of similarity among CDK family members makes the development of highly selective CDK2 inhibitors a great challenge. If the molecular selectivity is insufficient, it may lead to off-target phenomenon, which will affect the efficacy and safety of the drug.
With the assistance of the AI model Kinetic EnsemNET, Onson has successfully identified a key hidden dynamic binding pocket of CDK2, thereby developing a potential BIC CDK2 candidate with high activity, high selectivity and a wide therapeutic window, which lays the foundation for its subsequent collaboration with Beigene.
On the other hand, Ruge Pharmaceutical relied on its self-developed AI-assisted new drug research and development platform CARD to achieve the best selective screening of multiple CDK targets, and successfully promoted the clinical trial process of RGT-419B in the United States.
From the licensing trend of CDK inhibitors, we can take a lesson: in the future, investors may need to pay more attention to the investment opportunities of Biotech companies that use AI technology to solve the difficult drug target or hot target iterative drug development challenges.
Phase 1Clinical ResultLicense out/in
11 Sep 2024
NEW YORK--(
BUSINESS WIRE
)--Pfizer Inc. (NYSE: PFE) continues to showcase potential practice-changing research and next-generation candidates across its robust Oncology portfolio at the European Society for Medical Oncology (ESMO) Congress 2024, being held September 13-17 in Barcelona. Data from more than 50 company-sponsored, investigator-sponsored and collaborative research abstracts, including more than 10 oral and mini-oral presentations, will be presented across the company’s tumor areas and core scientific modalities, as well as a potential treatment for a cancer-related condition.
“
At this year’s ESMO, we are looking forward to demonstrating our progress toward delivering next-generation biologics and novel combinations that have the potential to be new standards of care for patients,” said Chris Boshoff, Chief Oncology Officer and Executive Vice President, Pfizer. “
Our key data presentations highlight our scientific leadership in developing targeted therapies, including small molecules and antibody-drug conjugates, across our core tumor areas, including breast, bladder and thoracic cancers.”
“
At ESMO, Pfizer will share important data highlighting our commitment to transforming outcomes for patients living with lung cancer, including longer-term follow-up results from the BRAFTOVI + MEKTOVI PHAROS study in
BRAF
V600E-mutated metastatic non-small cell lung cancer,” said Karin Tollefson, Chief Oncology Medical Officer, Pfizer. “
We are also looking forward to sharing progress on our industry-leading pipeline of new molecules, including encouraging early results for two novel, investigational antibody-drug conjugates and preliminary data on a novel combination of Pfizer’s next-generation CDK inhibitors.”
Key research includes a late-breaking presentation of updated results from the pivotal Phase 2 PHAROS* study of BRAFTOVI (encorafenib) + MEKTOVI (binimetinib) in patients with
BRAF
V600E-mutant metastatic non-small cell lung cancer (mNSCLC). Longer-term efficacy and safety data will be presented, following the initial primary overall response results (ORR) that supported the
FDA approval for BRAFTOVI + MEKTOVI in this indication in 2023
and the recent approval by the European Commission in August 2024. Further, Pfizer will share updated data from the safety lead-in of the ongoing Phase 3 BREAKWATER trial, showing antitumor activity of BRAFTOVI + cetuximab + FOLFIRI in patients with untreated
BRAF
V600E-mutant metastatic colorectal cancer (mCRC) in a mini-oral presentation.
Additionally, Pfizer will present a late-breaking Proffered Paper Presentation on the Phase 2 efficacy and safety results for its GDF-15 inhibitor, ponsegromab, in patients with cancer-associated cachexia, highlighting the company’s commitment to improving the treatment journey for people living with cancer. Cancer cachexia is a common, life-threatening wasting condition characterized by severe weight loss. The condition affects patients with advanced cancers and can greatly impact a patient’s ability to tolerate cancer treatment and quality of life. Despite its severity, there are no FDA-approved treatments for cachexia.
i,ii
Pfizer will also present early clinical-stage research for a number of priority pipeline areas, including encouraging Phase 1 results of the potential first-in-class antibody-drug conjugate (ADC) candidate SGN-PDL1V (PF-08046054)
in NSCLC and head and neck squamous cell carcinoma (HNSCC); initial data for the investigational ADC disitamab vedotin in combination with KEYTRUDA
®
(pembrolizumab) in human epidermal growth factor receptor 2 (HER2)-expressing locally advanced or metastatic urothelial cancer (la/mUC); and the first data combining atirmociclib, our highly-selective cyclin-dependent kinase 4 (CDK4) inhibitor (CDK4i), with a novel CDK2 inhibitor (CDK2i) in hormone receptor-positive (HR+)/HER2-negative metastatic breast cancer (MBC) from a Phase 1 dose-escalation study.
Key ESMO Presentations
Genitourinary Cancer
PADCEV + KEYTRUDA**:
additional analysis from the pivotal EV-302 trial continues to support the combination as a new standard of care for patients with previously untreated la/mUC. An exploratory analysis shows PADCEV + KEYTRUDA
®
showed consistent progression free survival (PFS), overall survival (OS), and ORR versus chemotherapy regardless of Nectin-4 or PD-L1 expression.
Disitamab Vedotin:
preliminary efficacy and safety data for disitamab vedotin in combination with KEYTRUDA highlights Pfizer’s continued commitment to developing novel therapeutics to meet the needs of patients with bladder cancer. Results from the safety run-in of the ongoing Phase 2 trial showed encouraging early efficacy and a safety profile consistent with previously presented data in treatment-naive patients with HER2-expressing la/mUC.
Thoracic Cancer
SGN-PDL1V (PF-08046054):
encouraging Phase 1 results will be presented for PDL1V, a novel, investigational vedotin ADC directed to PD-L1-expressing solid tumors. Data from the dose-escalation and dose optimization cohorts of the ongoing Phase 1 study show PDL1V as monotherapy was generally well tolerated with no unexpected adverse events, and encouraging antitumor activity was observed in patients with heavily pretreated NSCLC and HNSCC.
Breast Cancer
Atirmociclib (PF-07220060) + PF-07104091
: initial data from a dose-escalation study evaluating the innovative combination of atirmociclib, a potential first-in-class CDK4-selective inhibitor, with PF-07104091, a novel CDK2-selective inhibitor, showed a manageable safety profile and encouraging efficacy in patients with heavily pretreated HR+/HER2- breast cancer. These early results highlight the potential of Pfizer's strategy to advance atirmociclib as a future CDK inhibitor backbone therapy that may address treatment resistance with first generation CDK4/6i, subject to clinical success and regulatory approval. The CDK4i+2i combination is continuing to be explored in an ongoing Phase 1b/2 dose escalation and dose expansion study (NCT05262400).
Additional information on the Pfizer-sponsored abstracts, including date and time of presentation, follow in the chart below.
Pfizer is continuing its commitment to help non-scientists understand the latest findings with the development of abstract plain language summaries (APLS) for company-sponsored research being presented at ESMO, which are written in non-technical language. Those interested in learning more can visit
www.Pfizer.com/apls
to access the summaries starting September 16, 2024.
BREAST CANCER
Mini Oral Presentation (Abstract 618MO)
Saturday, September 14, 2:45 PM-4:15 PM CEST
Phase 1b/2 first-in-class novel combination trial of next generation CDK4-selective inhibitor PF-07220060 and next generation CDK2-selective inhibitor PF-07104091 in HR+ HER2- metastatic breast cancer and advanced solid tumors
Yap et al
Poster Presentation (Abstract 413P)
Monday, September 16, 9:00 AM-5:00 PM CEST
Longitudinal circulating tumor DNA (ctDNA) dynamics in Phase 1/2a study of the first-in-class CDK4-selective inhibitor, PF-07220060, in combination with endocrine therapy in patients with HR+/HER2− metastatic breast cancer (mBC) who progressed on prior CDK4/6 inhibitors
Yap et al
Poster Presentation (Abstract 359P)
Monday, September 16, 9:00 AM-5:00 PM CEST
Overall survival of palbociclib (PAL) + endocrine therapy (ET) in Japanese patients with hormone receptor-positive (HR+)/ human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer (ABC) in the 1st line (1L) or 2nd line (2L) setting: A multicenter observational study
Nakayama et al
Poster Presentation (Abstract 354P)
Monday, September 16, 9:00 AM-5:00 PM CEST
Synergistic preclinical efficacy through combination of the CDK4 and CDK2 selective inhibitors, PF-07220060 and PF-07104091, respectively, in HR+ HER2- breast cancer
Anders et al
Poster Presentation (Abstract 356P)
Monday, September 16, 9:00 AM-5:00 PM CEST
Real-world effectiveness in subgroups of palbociclib + endocrine therapy in HR+/HER2- ABC patients: Interim Results of the PERFORM study
Pfeiler et al
EARLY PIPELINE
Oral Presentation, Proffered Paper (Abstract 607O)
Friday, September 13, 4:00 PM-5:30 PM CEST
Interim results of a Phase 1 study of SGN-PDL1V (PF-08046054) in patients with PDL1-expressing solid tumors
Oliva Bernal et al
GASTROINTESTINAL CANCER
Mini Oral Presentation (Abstract 515MO)
Saturday, September 14, 2:45 PM-4:15 PM CEST
Encorafenib + cetuximab (EC) + FOLFIRI for
BRAF
V600E-mutant metastatic colorectal cancer (mCRC): updated results from the BREAKWATER safety lead-in (SLI)
Tabernero et al
GENITOURINARY CANCER
Mini Oral Presentation (Abstract 1966MO)
Sunday, September 15, 8:30 AM-10:00 AM CEST
EV-302: Exploratory analysis of nectin-4 expression and response to 1L enfortumab vedotin (EV) + pembrolizumab (P) in previously untreated locally advanced or metastatic urothelial cancer (la/mUC)
Powles et al
Poster Presentation (Abstract 1968P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Study EV-103 dose escalation/cohort A (DE/A): 5y follow-up of first-line (1L) enfortumab vedotin (EV) + pembrolizumab (P) in cisplatin (cis)-ineligible locally advanced or metastatic urothelial carcinoma (la/mUC)
Rosenberg et al
Poster Presentation (Abstract 2001P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Epidemiology and treatment patterns of patients with locally advanced or metastatic urothelial cancer in France: a non-interventional database study
Joly et al
Poster Presentation (Abstract 1638P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Enzalutamide (ENZA) with or without leuprolide in patients (pts) with high-risk biochemically recurrent (hrBCR) prostate cancer (PC): EMBARK post hoc analysis by age
Shore et al
Poster Presentation (Abstract 1626P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Incidence of hematologic toxicities in the homologous recombination repair (HRR)-deficient population of the TALAPRO-2 trial and their potential association with germline vs somatic origin of HRR gene alterations
Azad et al
Poster Presentation (Abstract 1637P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Efficacy of talazoparib and enzalutamide in metastatic castration-resistant prostate cancer (mCRPC) patients previously treated with androgen receptor pathway inhibitors (ARPI) or docetaxel – post hoc analysis from both cohorts in TALAPRO-2 study
Agarwal et al
Poster Presentation (Abstract 1633P)
Sunday, September 15, 9:00 AM-5:00 PM CEST
Phase 3 study of talazoparib (TALA) + enzalutamide (ENZA) vs placebo (PBO) + ENZA as first-line (1L) treatment in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC): TALAPRO-2 (TP-2) China cohort
Zeng et al
Mini Oral Presentation (Abstract 1967MO)
Sunday, September 15, 8:30 AM-10:00 AM CEST
Preliminary efficacy and safety of disitamab vedotin (DV) with pembrolizumab (P) in treatment (Tx)-naive HER2-expressing, locally advanced or metastatic urothelial carcinoma (la/mUC): RC48G001 Cohort C
Galsky et al
MELANOMA
Poster Presentation (Abstract 1071TiP)
Saturday, September 14, 9:00 AM-5:00 PM CEST
Phase 1 study of the investigational CD228 x 4-1BB costimulatory antibody Anticalin bispecific SGN-BB228 (PF-08046049) in advanced melanoma and other solid tumors
Dummer et al
SUPPORTIVE AND PALLIATIVE CARE
Oral Presentation, Proffered Paper (Abstract LBA82)
Saturday, September 14, 2:45 PM-4:25 PM CEST
Efficacy and safety of ponsegromab, a first-in-class, monoclonal antibody inhibitor of growth differentiation factor-15, in patients with cancer cachexia: A randomized, placebo-controlled, Phase 2 study
Crawford et al
THORACIC CANCER
Mini Oral Presentation (Abstract LBA56)
Saturday, September 14, 10:15 AM-11:45 AM CEST
Updated efficacy and safety from the Phase 2 PHAROS study of encorafenib plus binimetinib in patients with
BRAF
V600E-mutant metastatic NSCLC (mNSCLC)
Riely et al
Poster Presentation (Abstract 1398TiP)
Saturday, September 14, 9:00 AM-5:00 PM CEST
Be6A Lung-01, a Phase 3 study of sigvotatug vedotin (SV), an investigational antibody-drug conjugate (ADC) versus docetaxel in patients (pts) with previously treated non-small cell lung cancer (NSCLC)
Peters et al
Poster Presentation (Abstract 1279P)
Saturday, September 14, 9:00 AM-5:00 PM CEST
First-line lorlatinib vs crizotinib in Asian patients with ALK+ non-small cell lung cancer (NSCLC): 5-year outcomes from the CROWN study
Wu et al
*The PHAROS trial is conducted with support from Pierre Fabre.
**Pfizer and Astellas have a clinical collaboration agreement with Merck to evaluate the combination of PADCEV
®
and KEYTRUDA
®
in patients with previously untreated metastatic urothelial cancer.
Prescribing Information for Pfizer Medicines
Please see full
Prescribing Information
for PADCEV.
Please see full
Prescribing Information
for BRAFTOVI and full
Prescribing Information
for MEKTOVI.
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At Pfizer Oncology, we are at the forefront of a new era in cancer care. Our industry-leading portfolio and extensive pipeline includes three core mechanisms of action to attack cancer from multiple angles, including antibody-drug conjugates (ADCs), small molecules, bispecific antibodies and other immunotherapy biologics. We are focused on delivering transformative therapies in some of the world’s most common cancers, including breast cancer, genitourinary cancer, hematology-oncology, and thoracic cancers, which includes lung cancer. Driven by science, we are committed to accelerating breakthroughs that help people with cancer globally live better and longer lives.
About Pfizer: Breakthroughs That Change Patients’ Lives
At Pfizer, we apply science and our global resources to bring therapies to people that extend and significantly improve their lives. We strive to set the standard for quality, safety and value in the discovery, development and manufacture of health care products, including innovative medicines and vaccines. Every day, Pfizer colleagues work across developed and emerging markets to advance wellness, prevention, treatments and cures that challenge the most feared diseases of our time. Consistent with our responsibility as one of the world's premier innovative biopharmaceutical companies, we collaborate with health care providers, governments and local communities to support and expand access to reliable, affordable health care around the world. For 175 years, we have worked to make a difference for all who rely on us. We routinely post information that may be important to investors on our website at
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DISCLOSURE NOTICE:
The information contained in this release is as of September 11, 2024. The Company assumes no obligation to update forward-looking statements contained in this release as the result of new information or future events or developments.
This release contains forward-looking information about Pfizer Oncology, Pfizer’s Oncology portfolio of marketed and investigational therapies, including combinations, and an investigational therapy for a cancer-related condition; expectations for our product pipeline, in-line products and product candidates, including their potential benefits, clinical trial results and other developing data; potential breakthrough, best- or first-in-class or blockbuster status or expected market entry of our medicines; and other statements about our business, operations and financial results that involves substantial risks and uncertainties that could cause actual results to differ materially from those expressed or implied by such statements. Risk and uncertainties include, among other things, uncertainties regarding the commercial success of Pfizer’s oncology portfolio; the uncertainties inherent in research and development, including the ability to meet anticipated clinical endpoints, commencement and/or completion dates for our clinical trials, regulatory submission dates, regulatory approval dates and/or launch dates, as well as the possibility of unfavorable new clinical data and further analyses of existing clinical data; risks associated with interim and preliminary data; the risk that clinical trial data are subject to differing interpretations and assessments by regulatory authorities; whether regulatory authorities will be satisfied with the design of and results from our clinical studies; whether and when any drug applications, biologics license applications and/or emergency use authorization applications may be filed in any jurisdictions for any potential indication for Pfizer’s product candidates; whether and when any such applications that may be pending or filed for any of Pfizer’s product candidates may be approved by regulatory authorities, which will depend on myriad factors, including making a determination as to whether the product's benefits outweigh its known risks and determination of the product's efficacy and, if approved, whether any such product candidates will be commercially successful; decisions by regulatory authorities impacting labeling, manufacturing processes, safety and/or other matters that could affect the availability or commercial potential of Pfizer’s products or product candidates, including development of products or therapies by other companies; manufacturing capabilities or capacity; uncertainties regarding the impact of COVID-19 on Pfizer’s business, operations and financial results; and competitive developments.
A further description of risks and uncertainties can be found in Pfizer’s Annual Report on Form 10-K for the fiscal year ended December 31, 2023 and in its subsequent reports on Form 10-Q, including in the sections thereof captioned “Risk Factors” and “
Forward-Looking Information and Factors That May Affect Future Results”, as well as in its subsequent reports on Form 8-K, all of which are filed with the U.S. Securities and Exchange Commission and available at
www.sec.gov
and
www.pfizer.com
.
i
Cleveland Clinic. Cachexia (Wasting Syndrome).
Cachexia (Wasting Syndrome): Symptoms & Treatment (clevelandclinic.org)
. Accessed September 3, 2024.
ii
Lisa Martin, Michael B. Sawyer, Cancer Cachexia: Emerging Preclinical Evidence and the Pathway Forward to Clinical Trials,
JNCI: Journal of the National Cancer Institute
, Volume 107, Issue 12, December 2015, djv322,
https://doi.org/10.1093/jnci/djv322
Category: Pipeline
Clinical ResultPhase 1Phase 2Phase 3ADC
01 Jun 2023
Bayer has ceded a head start to its rivals for the CDK2 market.
Bayer is joining Blueprint Medicines, Incyte and Pfizer in the race to develop a selective CDK2 inhibitor, paying Cedilla Therapeutics an undisclosed sum for a preclinical challenger to the more advanced rivals.
Evidence that CDK2 is involved in processes that drive forms of breast, ovarian, uterine, stomach and esophageal cancers has spurred decades of research. Interest in the target intensified as it became clear that the kinase is implicated in changes that create breast cancers that are resistant to CDK4/6 inhibitors such as Pfizer’s Ibrance, Novartis’ Kisqali and Eli Lilly’s Verzenio.
CDK2 is a tough target, though, because researchers need to create molecules with selectivity against its isoforms to avoid an intolerable toxicity profile. Cedilla emerged as a biotech with a plan for how to beat the toxicity problem in 2021, when it disclosed its CDK2 program and raised $82.6 million.
Investors including RA Capital Management and Third Rock Ventures bet on Cedilla in the belief that its conditional inhibitors are a good fit for targets including CDK2. The inhibitors only modulate their targets when they are in a certain condition.
In the case of CDK2, the condition is binding to Cyclin E. Focusing on the Cyclin E1/CDK2 complex enabled Cedilla to identify a previously unreported binding site. If the biotech is right, targeting the binding site will improve on the selectivity of other CDK2 inhibitors and result in a more favorable risk-benefit profile.
Bayer has bought into the idea. In return for a financial package featuring upfront, milestone and royalty payments, the size of which remains under wraps, the German drugmaker has secured full rights to work on Cedilla’s Cyclin E1/CDK2 complex inhibitors. The Cedilla pipeline lists the program between preclinical and IND.
The upshot is Bayer has ceded a head start to its rivals for the CDK2 market. Pfizer is set to present phase 1/2a data on its candidate, PF-07104091, this week. Incyte and Blueprint Medicines joined Pfizer in the clinic last year, kicking off early-phase trials of INCB123667 and BLU-222, respectively. Blueprint was held up by a clinical hold but quickly fixed the problem and began working to resume enrollment in March.
100 Deals associated with Tagtociclib
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R&D Status
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Advanced Malignant Solid Neoplasm | Phase 2 | US | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | CN | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | AR | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | BR | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | BG | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | CZ | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | MX | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | ZA | 14 Mar 2022 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | ES | 14 Mar 2022 | |
| Breast Cancer | Phase 2 | US | 16 Sep 2020 |
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Clinical Result
Clinical Result
Indication
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Evaluation
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| Study | Phase | Population | Analyzed Enrollment | Group | Results | Evaluation | Publication Date |
|---|
NCT05262400 (ESMO2024) Manual  | Phase 1/2 | Advanced Malignant Solid Neoplasm | Hormone receptor positive HER2 negative breast cancer Hormone Receptor Positive | HER2 Negative | ESR1 Mutation | 33 | qjppopcigb(aopphagleo) = tlclmfweea vtcxnkwmgh (zkefzefdyg ) View more | Positive | 14 Sep 2024 | |
Phase 1 | - | 30 | (Treatment A: PF-07104091 Tablet Formulation A (Fasted)) | iizcrgsmuu(glcpoqiytr) = wttsrzhbck ycmpqxbiov (rdqengncep, sscevyqzqt - qmmkpipjux) View more | - | 08 Apr 2024 | |
(Treatment B: PF-07104091 Tablet Formulation B (Fasted)) | iizcrgsmuu(glcpoqiytr) = ublvwiuqgo ycmpqxbiov (rdqengncep, giwxvfsvet - shanghhljp) View more | ||||||
NCT04553133 (ASCO2023) Manual | Phase 1/2 | HR-positive/HER2-low Solid Tumors | Hormone receptor positive HER2 negative breast cancer Third line HR Positive | HER2 Negative | 35 | mphtotooec(hschnmcemq) = zxenezursj lxqvzccaip (icecwumxyo ) View more | Positive | 31 May 2023 |
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