Drugs / Mobocertinib
last change Jan 2025 re-read 2 minutes ago

Mobocertinib

Small molecule targets EGFR via inhibition

Developed for
non-small cell lung carcinoma
Investigated by
Millennium Pharmaceuticals, Inc. · Takeda

Regulatory milestones approvals, filings & regulatory actions · 1 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Approved US (FDA) EXKIVITY 2021-09-15 fda.gov

Trials 12 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 18 trials
Phase 1 NCT04056468 Oct 2020 → Feb 2022 Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT04441255 Jul → Aug 2020 Takeda Completed No outcome recorded
Phase 1 NCT04056455 Mar 2020 → Apr 2022 impaired renal function disease Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT04051827 Dec 2019 → Dec 2020 non-small cell lung carcinoma Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT03928327 May → Aug 2019 Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT03807778 Feb 2019 → Nov 2021 overdue non-small cell lung carcinoma Takeda Active not recruiting No outcome recorded
Phase 1 NCT03811834 Jan → Mar 2019 Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT03482453 Mar → Dec 2018 Millennium Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1/21 trial
Phase 1/2 NCT02716116 Jun 2016 → Oct 2026 expected non-small cell lung carcinoma Takeda Active not recruiting No outcome recorded
Phase 21 trial
Phase 2 NCT04576208 Nov 2020 → Jul 2022 non-small cell lung carcinoma Takeda Withdrawn No outcome recorded
Phase 31 trial
Phase 3 NCT04129502 Jan 2020 → Oct 2026 expected non-small cell lung carcinoma Takeda Active not recruiting No outcome recorded
Phase not stated1 trial
NCT04535557 non-small cell lung carcinoma Millennium Pharmaceuticals, Inc. Approved for marketing No outcome recorded

Press releases naming this drug 8 releases

DateIssuerRelease
2023-10-02 Takeda Takeda Provides Update on EXKIVITY® (mobocertinib) takeda.com
2023-01-11 Takeda Takeda’s EXKIVITY ® (mobocertinib) Receives Approval from the NMPA of China, Becoming the First and Only Therapy Available for Patients with EGFR Exon20 Insertion+ NSCLC takeda.com
2021-09-15 Takeda Takeda’s EXKIVITY™ (mobocertinib) Approved by U.S. FDA as the First Oral Therapy Specifically Designed for Patients with EGFR Exon20 Insertion+ NSCLC takeda.com
2021-05-19 Takeda Takeda Presents Updated Results for Mobocertinib, Further Substantiating the Clinical Benefit in Patients with EGFR Exon20 Insertion+ mNSCLC takeda.com
2021-04-27 Takeda Takeda Announces U.S. FDA Grants Priority Review for New Drug Application for Mobocertinib (TAK-788) as a Treatment for EGFR Exon20 Insertion+ Metastatic Non-Small Cell Lung Cancer takeda.com
2021-01-28 Takeda Takeda Presents Positive Results for Mobocertinib in Patients with EGFR Exon20 Insertion+ mNSCLC who Received Prior Platinum-Based Chemotherapy takeda.com
2020-04-27 Takeda Takeda Announces U.S. FDA Breakthrough Therapy Designation for Mobocertinib (TAK-788) for the Treatment of NSCLC Patients with EGFR Exon 20 Insertion Mutations takeda.com
2019-06-03 Takeda Takeda Presents Results from Lung Portfolio Including Phase 1/2 Study of TAK-788 in a Rare Form of NSCLC and New Data on Overall Health-Related Quality of Life for ALUNBRIG ® (brigatinib) takeda.com

Evidence & citations 11 cited values

Every value below carries the sentence it was read from. 16 sources stand behind the page.

FieldValueCited text
Known as Mobocertinib Mobocertinib is a kinase inhibitor designed to selectively target epidermal growth factor receptor (EGFR) exon 20 insertion (ex20ins) mutations in non-small cell lung cancer.” PMID 39815458 Jan 2025
6

“This study is about a medicine called TAK-788, also known as mobocertinib, given to adults with non-small cell lung cancer.” NCT02716116

NCT04056455

NCT04056468

NCT04535557

NCT03811834

NCT03807778

Known as AP-32788 ChEMBL registry synonym — accepted as the source's own label CHEMBL4650319
Known as AP-32788 SUCCINATE ChEMBL registry synonym — accepted as the source's own label CHEMBL4650319
Known as Exkivity ChEMBL registry synonym — accepted as the source's own label CHEMBL4650319
Known as MOBOCERTINIB SUCCINATE ChEMBL registry synonym — accepted as the source's own label CHEMBL4650319
Known as TAK-788 ClinicalTrials.gov intervention name — accepted as the source's own label NCT03928327
6

NCT04576208

NCT04051827

NCT04441255

NCT02716116

NCT03482453

NCT04129502

Known as TAK-788 SUCCINATE ChEMBL registry synonym — accepted as the source's own label CHEMBL4650319
Action Inhibit “oral inhibitor of EGFR exon 20 insertion mutations” PMID 38789848 May 2024
Modality Small molecule “Mobocertinib (TAK-788) is a first-in-class oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor” PMID 38789848 May 2024
Route Oral “This phase 1/2 study will evaluate the safety, pharmacokinetics, and anti-tumor activity of oral EGFR/HER2 Inhibitor TAK-788” NCT02716116
Target EGFR “Mobocertinib, an oral epidermal growth factor receptor (EGFR) inhibitor targeting EGFR gene mutations” PMID 33632775 Feb 2021