RegulationConditional marketing approval (CN), Fast Track (US), Orphan Drug (US), Breakthrough Therapy (CN), Priority Review (CN), Accelerated Approval (US)

Structure/Sequence

Molecular FormulaC36H45N7O8

InChIKeyYXYAEUMTJQGKHS-UHFFFAOYSA-N

CAS Registry2389149-74-8

Clinical Trials associated with Mobocertinib Succinate

NCT06441045

/ Not yet recruitingPhase 2IIT

Double Dose of Third-generation EGFR-TKI Plus Intrathecal Pemetrexed Versus Double Dose of Third-generation EGFR-TKI in NSCLC Patients With Leptomeningeal Progression Following the Treatment of Routine Dose of Third-generation EGFR-TKI: a Phase II Randomized, Multicenter Study

We aim to compare the efficacy and safety of double Dose of Third-generation EGFR-TKI Plus Intrathecal Pemetrexed Versus double Dose of Third-generation EGFR-TKI in patients with leptomeningeal progression following the treatment of routine dose of EGFR-TKI,

Start Date01 Oct 2024

Sponsor / Collaborator

Fujian Cancer Hospital

JPRN-UMIN000054805

/ SuspendedNot ApplicableIIT

Phase Ia/Ib Basket Trial on the safety and efficacy of Mobocertinib in combination with T-DM1 for patients with HER2 mutant solid tumors Biomarker study (WJOG16022MTR) - WJOG16022MTR

Start Date22 Jul 2024

Sponsor / Collaborator-

ChiCTR2400086657

/ SuspendedEarly Phase 1IIT

Randomized controlled clinical study of Traditional Chinese medicine detoxification and rash reduction granules (HQZ 60) for EGFR-TKI

Start Date10 Jul 2024

Sponsor / Collaborator-

100 Clinical Results associated with Mobocertinib Succinate

100 Translational Medicine associated with Mobocertinib Succinate

100 Patents (Medical) associated with Mobocertinib Succinate

5,907

Literatures (Medical) associated with Mobocertinib Succinate

01 Dec 2025·Cancer Chemotherapy and Pharmacology

Pharmacokinetics, mass balance, and metabolism of [14C]PLB1004, a selective and irreversible EGFR-TKI in humans

Article

Author: Diao, Xingxing ; Zhou, Haiyan ; Li, Weiqiang ; Zhang, Peilong ; Zhao, Wei ; Zhao, Furong ; Geng, Fei ; Liu, Donghui ; Zhang, Xinyue ; Ye, Panpan ; Gao, Lei ; Wang, Feiyu ; Yan, Shu ; Xue, Weizhe ; Li, Qian

PURPOSEPLB1004, developed by Beijing Avistone Biotechnology Co., Ltd., is a safe, highly selective, and efficient irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) employed in treating non-small-cell-lung-cancer (NSCLC). This study investigated its pharmacokinetics, mass balance, and metabolism in 6 healthy Chinese male subjects treated with 160 mg (70 µCi) [¹⁴C]PLB1004.METHODSFollowing drug administration, samples of blood, urine and feces were collected for quantitative determination of total radioactivity and metabolites were identified through radioactivity detection coupled with UHPLC-MS/MS.RESULTSFollowing drug administration, the median radioactive T_max was 4.17 h in plasma, with the average t_1/2 of PLB1004-related components in plasma of approximately 54.3 h. Over 264 h post-administration, the average cumulative excretion among the six subjects was 95.01% of the administered dose, with 84.71% and 10.30% excreted in feces and urine, respectively. Nine metabolites were characterized and identified and the parent drug PLB1004 was detected in plasma, urine, and feces. Among these metabolites, M689 was the most prevalent one in plasma, urine, and feces, constituting 25.37% of the total plasma radioactivity, and 55.88% and 1.73% of the administrated dose in feces and urine, respectively.CONCLUSIONFecal excretion emerged as PLB1004 excretion route, while urinary excretion via the kidneys served as the secondary route. The primarily metabolic pathways are oxidation, demethylation, dehydrogenation, and cysteine conjugation in humans.

01 Feb 2025·Biomedical Chromatography

A Simple and Sensitive LC‐MS/MS Method for the Determination of Mobocertinib and Its Metabolite Desmethyl‐Mobocertinib in Human Plasma and Its Application to Clinical Pharmacokinetic Study

Article

Author: Hou, Xiaoli ; Tang, Fan ; Cheng, Hong ; Cao, Yasen ; Chen, Jiajie ; Wang, Yixia

ABSTRACTMobocertinib is a potent selective tyrosine kinase inhibitor approved for the treatment of non–small cell lung cancer with activating EGFR exon 20 insertions. The aim of this study was to develop a procedure for liquid chromatography tandem mass spectrometry (LC‐MS/MS) for the determination of mobocertinib and its metabolite desmethyl‐mobocertinib in human plasma. The human plasma samples were precipitated with acetonitrile and analyzed using a Waters ACQUITY BEH C18 column coupled to a triple quadrupole mass spectrometer. Separation was executed using the acetonitrile–0.1% formic acid solution with gradient elution, at a flow rate of 0.4 mL/min. Mobocertinib and desmethyl‐mobocertinib were monitored by multiple reaction monitoring (MRM) with m/z 586.5 > 72.2 and 572.4 > 473.2, respectively. The procedure demonstrated excellent linearity (r > 0.997) within the concentration range of 0.1–200 ng/mL for both analytes. Precision in relative standard deviation was < 9.37% for mobocertinib and < 12.03% for desmethyl‐mobocertinib. Accuracy in relative error was within −7.23% to 9.18% for mobocertinib and −2.78% to 9.87% for desmethyl‐mobocertinib. Extraction recovery was > 80% for both analytes. The validated LC‐MS/MS method was successfully applied to the pharmacokinetic study of mobocertinib and desmethyl‐mobocertinib in healthy human volunteers with K2EDTA as anticoagulant after a single dose of mobocertinib (160 mg).

17 Jan 2025·Clinical Cancer Research

Aberrant Activation of Wound-Healing Programs within the Metastatic Niche Facilitates Lung Colonization by Osteosarcoma Cells

Article

Author: Jimenez Garcia, Leyre ; Cam, Maren ; Cannon, Matthew V. ; Reinecke, James B. ; Roberts, Ryan D. ; Gryder, Berkley E. ; Gross, Amy C. ; Dries, Ruben ; Gust, Matthew J. ; Sheridan, Jeffrey P.

AbstractPurpose:Lung metastasis is responsible for nearly all deaths caused by osteosarcoma, the most common pediatric bone tumor. How malignant bone cells coerce the lung microenvironment to support metastatic growth is unclear. The purpose of this study is to identify metastasis-specific therapeutic vulnerabilities by delineating the cellular and molecular mechanisms underlying osteosarcoma lung metastatic niche formation.Experimental Design:Using single-cell RNA sequencing, we characterized genome- and tissue-wide molecular changes induced within lung tissues by disseminated osteosarcoma cells in both immunocompetent murine models of metastasis and patient samples. We confirmed transcriptomic findings at the protein level and determined spatial relationships with multiparameter immunofluorescence and spatial transcriptomics. Based on these findings, we evaluated the ability of nintedanib, a kinase inhibitor used to treat patients with pulmonary fibrosis, to impair metastasis progression in both immunocompetent murine osteosarcoma and immunodeficient human xenograft models. Single-nucleus and spatial transcriptomics were used to perform molecular pharmacodynamic studies that define the effects of nintedanib on tumor and nontumor cells within the metastatic microenvironment.Results:Osteosarcoma cells induced acute alveolar epithelial injury upon lung dissemination. Single-cell RNA sequencing demonstrated that the surrounding lung stroma adopts a chronic, nonresolving wound-healing phenotype similar to that seen in other models of lung injury. Accordingly, the metastasis-associated lung demonstrated marked fibrosis, likely because of the accumulation of pathogenic, profibrotic, partially differentiated epithelial intermediates and macrophages. Our data demonstrated that nintedanib prevented metastatic progression in multiple murine and human xenograft models by inhibiting osteosarcoma-induced fibrosis.Conclusions:Fibrosis represents a targetable vulnerability to block the progression of osteosarcoma lung metastasis. Our data support a model wherein interactions between osteosarcoma cells and epithelial cells create a prometastatic niche by inducing tumor deposition of extracellular matrix proteins such as fibronectin that is disrupted by the antifibrotic tyrosine kinase inhibitor (TKI) nintedanib. Our data shed light on the non–cell-autonomous effects of TKIs on metastasis and provide a roadmap for using single-cell and spatial transcriptomics to define the mechanism of action of TKI on metastases in animal models.

159

News (Medical) associated with Mobocertinib Succinate

17 Jan 2025

·www.prnewswire.com

Innovent and ASK Pharm Jointly Announce NMPA Approval of Limertinib, a Third-generation EGFR TKI for the Treatment of Lung Cancer

SAN FRANCISCO and SUZHOU, China, Jan. 16, 2025 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of oncologic, autoimmune, cardiovascular and metabolic, ophthalmologic and other major diseases, and Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm, 002755.SZ), jointly announce that China's National Medical Products Administration (NMPA) has approved the New Drug Application (NDA) of limertinib for the treatment of adult patients with locally advanced or metastatic EGFR T790M-mutated non-small cell lung cancer (NSCLC). Limertinib is the 14th product in Innovent's commercial portfolio and represents a cutting-edge addition to its strong TKI franchise, offering an innovative precision therapy option to lung cancer patients. A Phase 2b pivotal study evaluating 301 patients with locally advanced or metastatic EGFR T790M-mutated NSCLC demonstrated limertinib's robust efficacy and safety profile. Independent review committee（IRC） assessment showed an overall response rate (ORR) of 68.8% and a disease control rate (DCR) of 92.4%. The median progression-free survival (PFS) reached 11.0 months, with a median duration of response (DoR) of 11.1 months. For patients with assessable central nervous system (CNS) lesions (N=99), the CNS best-ORR was 65.9% with a median PFS of 10.6 months. The safety profile aligned with other EGFR-targeting agents in its class. Additionally, limertinib met its primary endpoint in a Phase 3 clinical trial comparing it to gefitinib for first-line treatment of locally advanced or metastatic NSCLC harboring EGFR mutations. A separate NDA for the first-line treatment in adult patients with locally advanced or metastatic NSCLC carrying EGFR exon 19 deletions or exon 21 L858R mutations is currently under NMPA review. "Limertinib has demonstrated significant efficacy and safety in NSCLC patients with EGFR T790M mutation and EGFR-sensitive mutations. Patients treated with limertinib showed a reduced risk of CNS progression or death. This approval brings new hope and options to patients with advanced EGFR-mutated NSCLC in China," said Professor Shi Yuankai, MD, Department of Medical Oncology at Chinese Academy of Medical Sciences and Principal Investigator of the Phase 2b and Phase 3 clinical studies. Dr. Hui Zhou, Senior Vice President of Innovent, stated："The approval of limertinib's first indication marks a significant milestone, providing new treatment options for T790 mutation-positive lung cancer patients who have progressed after previous EGFR-TKI treatments. We anticipate the first-line treatment indication will benefit even more patients in the near future. As our 14th commercial product, limertinib represents an important advancement in precision medicine for lung cancer. We look forward to working with ASK Pharm to bring limertinib to market and benefit Chinese patients with EGFR-mutated NSCLC." Mr. Jingfei Ma, CEO and Executive Director of ASK Pharm, stated: "Beyond the approval for EGFR T790M+ NSCLC, limertinib is also under regulatory review for first-line treatment of EGFR 19DEL+ or L858R+ NSCLC in China. ASKC202, a new highly selective c-Met inhibitor, is currently undergoing clinical study in combination with limertinib to treat patients with third-generation EGFR-TKI resistance. Together with Innovent, we look forward to limertinib benefiting more Chinese lung cancer patients in the near future. The first approval of limertinib, a Class I innovative product, represents significant progress in the company's transformation toward innovative drug research and development. " About EGFR mutation-positive non-small-cell lung cancer (NSCLC) Lung cancer remains one of the deadliest and most common cancers globally[i], with NSCLC accounting for about 85% of cases. Around 70% of NSCLC patients are diagnosed at locally advanced or metastatic disease stages that cannot be surgically resected. EGFR mutations are particularly prevalent in Asian NSCLC patients, affecting 30% to 50% of cases. EGFR-TKIs are the recommended first-line standard of care for this group, with third-generation EGFR inhibitors offering the broadest applicability. About Limertinib Limertinib is an orally-administrated, third-generation EGFR TKI with proprietary rights, approved by the China's NMPA for the treatment of adult patients with locally advanced or metastatic EGFR T790M-mutated non-small cell lung cancer (NSCLC). A second NDA is under NMPA review for first-line treatment of adult patients with locally advanced or metastatic NSCLC carrying EGFR exon 19 deletions or exon 21 L858R mutations. The drug demonstrated success in a multi-center, randomized, double-blind, controlled Phase 3 clinical trial comparing its efficacy and safety of to gefitinib in first-line treatment of patients with locally advanced or metastatic NSCLC harboring EGFR mutations. With the primary endpoint met, results will be presented at upcoming academic conferences or published in academic journals. In October 2024, Innovent and ASK Pharm entered into a strategic collaboration and license agreement for limertinib in Mainland China. About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 14 products in the market. It has 3 new drug applications (NDA) under regulatory review, 3 assets in Phase III or pivotal clinical trials and 17 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli Lilly, Sanofi, Incyte, Adimab, LG Chem and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. About Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm) Founded in January 2003, Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm) is a research-based pharmaceutical enterprise that integrates and streamlines innovative research and development with manufacture, marketing promotion and sales of proprietary pharmaceuticals, fine chemicals and health-care products. ASK Pharm specializes in digestive disease, multidrug resistant infection, oncology and chronic disease areas. ASK Pharm focuses on the R&D of small-molecule targeted innovative drugs and immuno-oncology biologic drugs. Currently, there are 48 major research projects, including 11 disclosed key projects focused on innovative chemical and biologic drugs. Among these, the innovative anti-tumor drug Limertinib are in the NDA stage, while ASKC109 (maltol iron capsules) and ASKB589 (Claudin18.2 monoclonal antibody) are in Phase III clinical trials. ASK Pharm has Ranked among the top 20 best industrial enterprises in China's pharmaceutical R&D pipeline for 14 consecutive years and it has also received numerous honors such as "Top Ten National R&D Innovators", "Best National Enterprise for Investment", and "National Torch Program High-Tech Enterprises". For more information, visit . Innovent's Forward-Looking Statements This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent, are intended to identify certain of such forward-looking statements. Innovent does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of Innovent with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond Innovent's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, Innovent's competitive environment and political, economic, legal and social conditions. Reference SOURCE Innovent Biologics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Clinical ResultPhase 2Phase 3License out/inDrug Approval

02 Jan 2025

·pmlive.com

J&J’s Rybrevant/Lazcluze combination approved by EC for EGFR-mutated lung cancer

Johnson & Johnson (J&J) has announced that its chemotherapy-free combination has been approved by the European Commission (EC) for a subset of epidermal growth factor receptor (EGFR)-mutated lung cancer patients. Rybrevant (amivantamab), an EGFR-MET bispecific antibody, plus Lazcluze (lazertinib), a third-generation EGFR tyrosine kinase inhibitor (TKI), has been approved for the first-line treatment of adults with advanced non-small cell lung cancer (NSCLC) with EGFR exon 19 deletions or exon 21 L858R substitution mutations. The EC’s decision was based on positive results from the late-stage MARIPOSA study, which compared Rybrevant plus Lazcluze against the current first-line standard of care, AstraZeneca’s own third-generation EGFR-TKI Tagrisso (osimertinib), in this patient population. The trial met its primary endpoint, with J&J’s combination demonstrating a 30% reduction in the risk of disease progression or death compared to Tagrisso at a median follow-up of 22 months. The median duration of response was also longer for patients receiving Rybrevant plus Lazcluze compared to Tagrisso, at 25.8 versus 16.8 months, and the safety profile of the combination was consistent with previous reports from phase 1 to 2 studies. NSCLC accounts for up to 85% of all lung cancer cases, and alterations in EGFR are among the most common driver mutations in patients with this form of the disease. Patients are often treated with EGFR TKIs. However, treatment resistance and disease recurrence remains a significant challenge and there is an urgent need for alternative targeted therapies earlier in the treatment pathway, according to J&J. Henar Hevia, senior director, EMEA therapeutic area lead, oncology, J&J Innovative Medicine, said the EC’s approval “marks significant progress for those living with the devastating impact of EGFR-mutated NSCLC, who too often face a poor prognosis and limited treatment options”. “The combination of [Rybrevant] and [Lazcluze] exemplifies the potential of targeted precision medicine, offering a tailored approach that addresses the underlying genetic drivers of the disease, and avoids or delays the need for chemotherapy,” she said. The decision comes just over four months after the EC approved Rybrevant for use alongside carboplatin and pemetrexed chemotherapy to treat advanced NSCLC in adults with EGFR exon 19 deletions or exon 21 L858R substitution mutations who have failed on prior therapy, including an EGFR TKI.

Clinical ResultDrug Approval

23 Dec 2024

·pipelinereview.com

Tagrisso approved in the EU for patients with unresectable EGFR-mutated lung cancer

First and only EGFR inhibitor and targeted treatment approved in the EU in unresectable NSCLC Approval based on LAURA Phase III trial results which showed Tagrisso extended median progression-free survival to more than three years LONDON, UK I December 23, 2024 I AstraZeneca’s Tagrisso (osimertinib) has been approved in the European Union (EU) for the treatment of adult patients with locally advanced, unresectable non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor ( EGFR ) exon 19 deletions or exon 21 (L858R) substitution mutations and whose disease has not progressed during or following platinum-based chemoradiation therapy (CRT). The approval by the European Commission follows the positive opinion of the Committee for Medicinal Products for Human Use and is based on results from the LAURA Phase III trial, which were published in The New England Journal of Medicine . In the trial, Tagrisso reduced the risk of disease progression or death by 84% compared to placebo (hazard ratio 0.16; 95% confidence interval 0.10-0.24; p<0.001) as assessed by blinded independent central review. Median progression-free survival (PFS) was 39.1 months in patients treated with Tagrisso versus 5.6 months for placebo. Overall survival (OS) results remain immature, and the trial is continuing to assess OS as a secondary endpoint. Each year in Europe, there are more than 450,000 people diagnosed with lung cancer, and approximately 80-85% have NSCLC. 1-3 Among those with NSCLC in Europe, about 10-15% have tumours with an EGFR mutation. 4-6 Manuel Cobo, MD, Specialist Physician of the Medical Oncology Service at the Carlos Haya University Hospital, Malaga, Spain, and investigator for the trial, said: “Today’s approval marks a major breakthrough for patients in the EU with unresectable, EGFR -mutated non-small cell lung cancer, delivering the first targeted treatment in this setting. Osimertinib reduced the risk of disease progression or death by an unprecedented 84 per cent in the LAURA trial, setting a new benchmark for outcomes and underscoring the importance of testing for EGFR mutations upon diagnosis.” Dave Fredrickson, Executive Vice President, Oncology Business Unit, AstraZeneca, said: “ Tagrisso is now the first and only EGFR inhibitor and targeted treatment approved in the EU for locally advanced, unresectable lung cancer, providing a new standard of care to patients who have historically experienced early progression after chemoradiation therapy. The powerful results from the LAURA trial show Tagrisso improves outcomes for patients in the unresectable setting, reinforces the importance of timely EGFR testing and solidifies Tagrisso as the backbone therapy in EGFR -mutated non-small cell lung cancer.” The safety and tolerability of Tagrisso in the LAURA trial was consistent with its established profile and no new safety concerns were identified. This is the fifth major approval for Tagrisso based on the LAURA trial following recent approvals in the US, Switzerland, South Korea and Australia. Regulatory applications are also currently under review in China, Japan and several other countries. Tagrisso is approved as monotherapy in more than 100 countries including in the US, EU, China and Japan. Approved indications include 1st-line treatment of patients with locally advanced or metastatic EGFR m NSCLC, locally advanced or metastatic EGFR T790M mutation-positive NSCLC, and adjuvant treatment of early-stage EGFR m NSCLC. Tagrisso is also approved in combination with chemotherapy in the US, China and several other countries for 1st-line treatment of patients with locally advanced or metastatic EGFR m NSCLC. Notes Lung cancer Each year, an estimated 2.4 million people are diagnosed with lung cancer globally. 7 Lung cancer is the leading cause of cancer death among both men and women, accounting for about one-fifth of all cancer deaths. 7 Lung cancer is broadly split into NSCLC and small cell lung cancer, with 80-85% of patients diagnosed with NSCLC, the most common form of lung cancer. 2,3 The majority of all NSCLC patients are diagnosed with advanced disease. 8 Approximately 10-15% of NSCLC patients in the US and Europe, and 30-40% of patients in Asia have EGFR m NSCLC. 4-6 Patients with EGFR m NSCLC are particularly sensitive to treatment with an EGFR -tyrosine kinase inhibitor ( EGFR -TKI) which blocks the cell-signalling pathways that drive the growth of tumour cells. 9 LAURA LAURA is a randomised, double-blind, placebo-controlled, multi-centre, global Phase III trial in patients with unresectable, Stage III EGFR m NSCLC whose disease has not progressed following definitive platinum‑based CRT. Patients were treated with Tagrisso 80mg once-daily oral tablets until disease progression, unacceptable toxicity or other discontinuation criteria were met. Upon progression, patients in the placebo arm were offered treatment with Tagrisso . The trial enrolled 216 patients in more than 145 centres across more than 15 countries, including in the US, Europe, South America and Asia. The primary endpoint is PFS. The trial is ongoing and will continue to assess the secondary endpoint of OS. Tagrisso Tagrisso (osimertinib) is a third-generation, irreversible EGFR -TKI with proven clinical activity in NSCLC, including against central nervous system metastases. Tagrisso (40mg and 80mg once-daily oral tablets) has been used to treat patients across its indications worldwide and AstraZeneca continues to explore Tagrisso as a treatment for patients across multiple stages of EGFR m NSCLC. There is an extensive body of evidence supporting the use of Tagrisso as standard of care in EGFR m NSCLC. Tagrisso improved patient outcomes in early-stage disease in the ADAURA Phase III trial , Stage III, unresectable disease in the LAURA Phase III trial , late-stage disease in the FLAURA Phase III trial , and with chemotherapy in the FLAURA2 Phase III trial . As part of AstraZeneca’s ongoing commitment to treating patients as early as possible in lung cancer, Tagrisso is also being investigated in the neoadjuvant setting in the NeoADAURA Phase III trial and in the early-stage adjuvant resectable setting in the ADAURA2 Phase III trial. The Company is also researching ways to address tumour mechanisms of resistance through the SAVANNAH and ORCHARD Phase II trials, and the SAFFRON Phase III trial, which test Tagrisso plus savolitinib as well as other potential new medicines. AstraZeneca in lung cancer AstraZeneca is working to bring patients with lung cancer closer to cure through the detection and treatment of early-stage disease, while also pushing the boundaries of science to improve outcomes in the resistant and advanced settings. By defining new therapeutic targets and investigating innovative approaches, the Company aims to match medicines to the patients who can benefit most. The Company’s comprehensive portfolio includes leading lung cancer medicines and the next wave of innovations, including Tagrisso and Iressa (gefitinib); Imfinzi (durvalumab) and Imjudo (tremelimumab); Enhertu (trastuzumab deruxtecan) and datopotamab deruxtecan in collaboration with Daiichi Sankyo; Orpathys (savolitinib) in collaboration with HUTCHMED; as well as a pipeline of potential new medicines and combinations across diverse mechanisms of action. AstraZeneca is a founding member of the Lung Ambition Alliance, a global coalition working to accelerate innovation and deliver meaningful improvements for people with lung cancer, including and beyond treatment. AstraZeneca in oncology AstraZeneca is leading a revolution in oncology with the ambition to provide cures for cancer in every form, following the science to understand cancer and all its complexities to discover, develop and deliver life-changing medicines to patients. The Company’s focus is on some of the most challenging cancers. It is through persistent innovation that AstraZeneca has built one of the most diverse portfolios and pipelines in the industry, with the potential to catalyse changes in the practice of medicine and transform the patient experience. AstraZeneca has the vision to redefine cancer care and, one day, eliminate cancer as a cause of death. AstraZeneca AstraZeneca (LSE/STO/Nasdaq: AZN) is a global, science-led biopharmaceutical company that focuses on the discovery, development, and commercialisation of prescription medicines in Oncology, Rare Diseases, and BioPharmaceuticals, including Cardiovascular, Renal & Metabolism, and Respiratory & Immunology. Based in Cambridge, UK, AstraZeneca’s innovative medicines are sold in more than 125 countries and used by millions of patients worldwide. Please visit astrazeneca.com and follow the Company on social media @AstraZeneca . References SOURCE: AstraZeneca

Phase 3Clinical ResultDrug Approval

100 Deals associated with Mobocertinib Succinate

External Link

KEGG	Wiki	ATC	Drug Bank
D11969	-	-	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
EGFR ex20ins mutation in non-small cell lung cancer	AU	Takeda Pharmaceuticals Australia Pty Ltd.	19 Jul 2022

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
EGFR ex20ins mutation in non-small cell lung cancer	Phase 2	US	Takeda Pharmaceuticals U.S.A., Inc.	15 Sep 2021
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	TW	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	US	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	KR	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	GB	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	JP	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	DE	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	ES	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	CN	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


JPRN-jRCT2051220070 (WJOG16022M, ASCO2024)	Phase 1	Solid tumor HER2 mutations	28	Mobocertinib 80 mg	udunfpsvgs(ltfutyjrkk) = grade ≥ 3 AE occurred in 72.7% of pts; the common events (>5%) being thrombocytopenia (50.0%), diarrhea (13.6%), and anorexia (13.6%) eusdeyekrx (xivqqemtdm )	Positive	24 May 2024
NCT03811834 (phase 1 study, Pubmed)	Phase 1	EGFR exon 20 insertion mutations	-	Mobocertinib 160 mg	nbdsiwnzqr(vpasccerox) = all adverse events were Grade 1 in severity okymfirckw (gigsfvsiyv )	-	24 May 2024
				[14C]-Mobocertinib 50 µg
NCT04051827 (CTgov)	Phase 1	Advanced Lung Non-Small Cell Carcinoma	26	Midazolam (Part A: Midazolam Alone)	tkfaupjqvz(seiqwuiipz) = bphtivqtym fuvnosrckb (xnnvfmptzk, gorlwzlcov - xigcawuyxv) View more	-	12 Apr 2024
				Midazolam+Mobocertinib (Part A: Midazolam + Mobocertinib)	tkfaupjqvz(seiqwuiipz) = vlaagnbtcj fuvnosrckb (xnnvfmptzk, lssbrizxag - soyhprlgwc) View more
NCT04056455 (CTgov)	Phase 1	Neoplasms	26	Mobocertinib (Severe Renal Impairment: Mobocertinib 80 mg)	wbttoodmdp(idxbhyrvkb) = popcjojscn dyrzwjjlbo (wuttqsqoaj, wyyzfakrtg - bgsuwzgmgu) View more	-	08 Jan 2024
				Mobocertinib (Normal Renal Function: Mobocertinib 80 mg)	wbttoodmdp(idxbhyrvkb) = mtgyumkgdg dyrzwjjlbo (wuttqsqoaj, kappjfdnci - qevrzjntlz) View more
NCT02716116 (ESMO_ASIA2023)	Phase 1/2	Non-Small Cell Lung Cancer EGFR ex20ins-positive	57	mobocertinib	(jdywhsrbbo) = sigympoqvg dliufxbwvw (akntzidkrl ) View more	-	02 Dec 2023
ESMO_ASIA2023	Not Applicable	EGFR-mutated non-small Cell Lung Cancer EGFR exon 20 insertion mutations	105	Mobocertinib	(kzudvvcbug) = 51 patients (48.6%) reported diarrhea (all grades) related to mobocertinib (treatment discontinuation due to diarrhea: 4 patients [7.8%]) tvxufjkpvc (gfczdhljww )	Positive	02 Dec 2023
NCT04056468 (CTgov)	Phase 1	Liver Injury	24	Mobocertinib (Moderate HI (Child-Pugh B): Mobocertinib 40 mg)	plenlkjhba(lbbpikqfni) = gzxoliojmw sesmwdrxnw (vmcofnrtpm, hitizvaqdk - jieefwnpvz) View more	-	03 Nov 2023
				Mobocertinib (Severe HI (Child-Pugh C): Mobocertinib 40 mg)	plenlkjhba(lbbpikqfni) = bujenpuxhy sesmwdrxnw (vmcofnrtpm, spjhjlronb - nmjznwoppc) View more
NCT03807778 (CTgov)	Phase 1	Non-Small Cell Lung Cancer	53	Mobocertinib (Mobocertinib, Phase 1 Part: All Participants)	faemgfesfg(rutwyzvqck) = ufifpqagua nfteqjuavs (fzttfozeps, ingmdmwcfx - inlbfzeyrh) View more	-	03 Oct 2023
				Mobocertinib (Mobocertinib 160 mg, Phase 2 Part)	cjvqowcpzp(xwlekqunae) = hefoitbmcb rshpfqtynd (adcuwgaxmt, wuoyhgtbwn - uuarpmhdbp) View more
NCT04129502 (EXCLAIM-2, Corporate Publications) Manual	Phase 3	Non-Small Cell Lung Cancer First line	-	EXKIVITY	(zqeocoholl) = No new safety signals were observed in the EXCLAIM-2 trial. gqrrbemwjj (nntffxzklx ) View more	Negative	02 Oct 2023
				platinum-based chemotherapy
NCT02716116 (ASCO2023) Manual	Phase 1/2	EGFR ex20ins mutation in non-small cell lung cancer EGFR exon 20 insertion mutations	114	Mobocertinib (patients who tested EGFR ex20ins positive by F1LCDX)	(qscucbccqo) = bmblopnokg ncsyljbzvn (yhakauemzg ) View more	Positive	31 May 2023
				Mobocertinib (all EGFR ex20ins–positive platinum-pretreated patients)	(qscucbccqo) = ozxvvicpfs ncsyljbzvn (yhakauemzg ) View more

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