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Afatinib: First Global Approval
DOI:10.1007/s40265-013-0111-6.png)
摘要
En 中文
Afatinib, an irreversible inhibitor of the ErbB family of tyrosine kinases, is under development with Boehringer Ingelheim for the once-daily, oral treatment of cancer. Afatinib downregulates ErbB signalling by covalently binding to epidermal growth factor receptor (EGFR), human epidermal growth factor receptor (HER) 2 and HER4, irreversibly inhibiting tyrosine kinase autophosphorylation. It also inhibits transphosphorylation of HER3. Oral afatinib (Gilotrif (TM)) has been approved in the US for the first-line treatment of patients with metastatic non-small-cell lung cancer (NSCLC) who have tumours with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by a US FDA-approved test. Afatinib has also been approved in Taiwan for the first-line treatment of patients with EGFR mutation-positive NSCLC. In addition, the European Medicines Agency's Committee for Medicinal Products for Human Use has recommended the approval of afatinib (Giotrif(A (R))) for the treatment of patients with locally advanced or metastatic NSCLC with activating EGFR mutations who are EGFR tyrosine kinase inhibitor na < ve. Afatinib is also under regulatory review in Canada, Japan and other Asian countries. This article summarizes the milestones in the development of afatinib, leading to this first approval in patients with metastatic NSCLC.
Keyword:
CELL LUNG-CANCER
GROWTH-FACTOR RECEPTOR
ERBB FAMILY BLOCKER
I DOSE-ESCALATION
BIBW 2992
PHASE-I
OPEN-LABEL
TYROSINE KINASE
ORAL TREATMENT
TRIAL
AI总结
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期刊
IF:
14.4
论文数:
8.4K
被引数:
2.3W
机构
引用论文
LUX-Breast 3: Randomized Phase II trial of afatinib (BIBW 2992) alone or with vinorelbine versus investigator's choice of treatment in patients (pts) with HER2-positive breast cancer (BC) with progressive brain metastases after trastuzumab and/or lapatinib-based therapy*
CANCER RESEARCH
IF16.6
LUX-Breast 2: Phase II, open-label study of oral afatinib in HER2-overexpressing metastatic breast cancer (MBC) patients (pts) who progressed on prior trastuzumab and/or lapatinib
CANCER RESEARCH
IF16.6
Open-label, Phase II trial of afatinib, with or without vinorelbine, for the treatment of HER2-overexpressing inflammatory breast cancer (IBC)
CANCER RESEARCH
IF16.6

