Drug · Small Molecule

Afatinib

CI-DRUG-00000043Explore in graph →NCIt C66940 CHEMBL1173655 CIViC Approved

Regulatory

Approvals (20)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory20 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as MAR-AFATINIB (DIN 02517035) under ATC L01EB03 AFATINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Jan 31, 2025	health-canada-dpd
CA

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 2 days agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	19	10	17	146	20	CA, EU, US	Jul 12, 2013	2003-11
Malignant Lung Neoplasm	Approved	Phase 4	4	1	11	50	3	EU, US	Jul 12, 2013	2007-08
Multiple Myeloma	Phase2	Phase 2	3	0	0	4	0	—	—	Aug 12, 2015
Non-Hodgkin Lymphoma	Phase2	Phase 2	3	0	0	4	0	—

Curated evidence

Clinical evidence (132)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 132 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
NRG1 Fusion1
Afatinib	Cholangiocarcinoma

Clinical trials

Trials with this intervention (163)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 51–100 of 163 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT02183883	Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity(DARWIN1)	completed	Phase 2	12	University College, LondonOTHER	1	Nov 29, 2023	clinicaltrials
NCT03088059	Biomarker-based Study in R/M SCCHN(UPSTREAM)	unknown

Molecule

Record

Kind: Small Molecule
Mechanism: Epidermal growth factor receptor erbB1 inhibitor; Receptor protein-tyrosine kinase erbB-2 inhibitor; Receptor protein-tyrosine kinase erbB-4 inhibitor
Targets: 3 genes
UNII: V1T5K7RZ0B
Aliases: (2e)-N-(4-(3-Chloro-4-Fluoroanilino)-7-(((3s)-Oxolan-3-yl)Oxy)Quinoxazolin-6-yl)-4-(Dimethylamino)But-2-Enamide, Afatinib, AFATINIB (BIBW2992), Afatinib Dimaleate, AFATINIB DIMALEATE, AFATINIB FREE BASE, BIBW 2992, BIBW-2992, BIBW2992, BIBW2992 (AFATINIB), BIBW2992AFATINIBTOVOKS1011, BIBW2992-MA2, (E/Z)-AFATINIB, (E/Z)-BIBW 2992, GILOTRIF, Giotrif, GIOTRIF, MAR-AFATINIB, NSC-750691, SANDOZ AFATINIB, TEVA-AFATINIB, TOMTOVOK, TOVOK

Data updated 22 hours agoSource updated unknown

Identifiers

Codes (27)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EB03	AFATINIB
ATC (WHO)	L01XE13

EGFR G598V2
Afatinib + Erlotinib + OsimertinibSubstitutes	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	submitted	EID8234 Patient-derived GBM brain tumour stem cells (BTSCs) were used to test the efficacy of EGFR inhibitors in vitro. Afatinib inhibited the growth and sphere-forming ability of BTSCs but not normal astrocy… (full text at CIViC) PMID 32226941 · Jensen et al., 2020 · Open in CIViC	civic
Afatinib + PacritinibCombination	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID8235 Patient-derived GBM brain tumour stem cells (BTSCs) were used to test the efficacy of the EGFR inhibitor afatinib and JAK2 inhibitor pacritinib in vitro. Combination treatment with afatinib and pacrit… (full text at CIViC) PMID 32226941 · Jensen et al., 2020 · Open in CIViC	civic

EGFR VIII2
Afatinib	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	4	submitted	EID8191 Patient-derived GBM brain tumour stem cells (BTSCs) were used to test the efficacy of the EGFR inhibitor afatinib in vitro and in vivo. Afatinib inhibited the growth and sphere-forming ability of BTSC… (full text at CIViC) PMID 32226941 · Jensen et al., 2020 · Open in CIViC	civic
Afatinib + PacritinibCombination	GlioblastomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	submitted	EID8192 Patient-derived GBM brain tumour stem cells (BTSCs) were used to test the efficacy of the EGFR inhibitor afatinib and JAK2 inhibitor pacritinib in vitro and in vivo. Combination treatment with subopti… (full text at CIViC) PMID 32226941 · Jensen et al., 2020 · Open in CIViC	civic

ERBB2 Amplification6
Afatinib	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	3	accepted	EID961 A phase II study involving adult female patients, >=18 years, with stage IIIB or IV HER2-positive (by IHC and/or in situ fluorescence) metastatic breast cancer. All patients were previously treated wi… (full text at CIViC) PMID 22418700 · Lin et al., 2012 · Open in CIViC	civic
〃	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	3	rejected	EID1010 With multiple mechanisms of HER reprogramming thought to be behind trastuzumab resistance, including increased expression of ErbB members, afatinib, which broadly and irreversibly targets ErbB recepto… (full text at CIViC) PMID 22418700 · Lin et al., 2012 · Open in CIViC	civic
〃	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	3	accepted	EID1011 This Phase II trial (LUX-Breast 3 - NCT01441596) compared afatinib, afatinib plus vinorelbine, or investigator's choice of treatment. 121 patients with HER2 overexpressing breast cancer with CNS recu… (full text at CIViC) PMID 26596672 · Cortés et al., 2015 · Open in CIViC	civic
〃	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Does Not Support Sensitivity Response	4	accepted	EID1012 LUX-Breast 1 is a phase 3 trial (NCT01125566) which enrolled 508 patients with metastatic HER2 positive BC who had progressed after adjuvant or first-line trastuzumab. It was thought that the wider ra… (full text at CIViC) PMID 26822398 · Harbeck et al., 2016 · Open in CIViC	civic
Afatinib + Lapatinib + TrastuzumabSubstitutes	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	2	accepted	EID887 In this phase 2 trial, treatment-naive, ERBB2-positive (by IHC) breast cancer patients with stage IIIA, B, C or inflammatory disease were randomized 1:1:1 to afatinib (n = 10), lapatinib (n = 8), or t… (full text at CIViC) PMID 25537159 · Rimawi et al., 2015 · Open in CIViC	civic
Afatinib + TrastuzumabCombination	HER2-Positive Breast CarcinomaALIAS	Predictive	B	Supports Sensitivity Response	3	accepted	EID1013 Trastuzumab resistance is thought to consist of multiple compensatory mechanisms involving ErbB family members such as increased signaling through ErbB family heterodimers. The irreversible TKI afati… (full text at CIViC) PMID 25370464 · Ring et al., 2015 · Open in CIViC	civic

EGFR Exon 19 Deletion4
Afatinib	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID880 A phase III clinical trial (NCT00949650) found that median progression free survival among patients with EGFR exon 19 deletion was 13.6 months for afatinib and 6.9 months for chemotherapy (HR, 0.47; 9… (full text at CIViC) PMID 23816960 · Sequist et al., 2013 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID882 In a phase 2 study (NCT00525148), patients with lung adenocarcinoma (stage IIIb with pleural effusion or stage IV) and EGFR mutations, treated with afatinib, were assessed by objective response. In to… (full text at CIViC) PMID 22452895 · Yang et al., 2012 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID981 Afatinib is an irreversible covalent inhibitor of EGFR (second generation). This Phase III clinical trial (LUX-Lung 6; NCT01121393) was performed in Asian patients with EGFR mutant advanced NSCLC. 364… (full text at CIViC) PMID 24439929 · Wu et al., 2014 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID983 In analysis of LUX-Lung 3 and LUX-Lung 6 trials (NCT00949650 and NCT01121393), of EGFR mutant NSCLC, median overall survival with afatinib treatment was seen to be significantly improved over chemothe… (full text at CIViC) PMID 25589191 · Yang et al., 2015 · Open in CIViC	civic

EGFR L858R3
Afatinib	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID879 A phase III clinical trial (NCT00949650) found that median progression free survival among patients with exon 19 deletions or L858R EGFR mutations (n = 308) was 13.6 months for afatinib and 6.9 months… (full text at CIViC) PMID 23816960 · Sequist et al., 2013 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	3	accepted	EID883 In a phase 2 study of patients with lung adenocarcinoma (stage IIIb with pleural effusion or stage IV) and EGFR mutations, treated with afatinib were assessed by objective response. 129 patients were … (full text at CIViC) PMID 22452895 · Yang et al., 2012 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID982 Afatinib is an irreversible covalent inhibitor of EGFR (second generation). This Phase III clinical trial (LUX-Lung 6; NCT01121393) was performed in Asian patients with EGFR mutant advanced NSCLC. 364… (full text at CIViC) PMID 24439929 · Wu et al., 2014 · Open in CIViC	civic

EGFR E746_A750del2
Afatinib	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	—	submitted	EID2515 In a phase 2b/3 study of 585 lung adenocarcinoma patients who had a previous round of EGFR-TKI treatment, archival material was available for 141 patients. EGFR mutational analysis revealed that 96 tu… (full text at CIViC) PMID 22452896 · Miller et al., 2012 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	—	submitted	EID2516 A phase 3 study of 345 stage IIIB-IV lung adenocarcinoma patients, reported improved median progression free survival (13.6 months vs. 6.9 months, HR: 0.47, 95% CI: 0.34-0.65, P=0.001) in EGFR mutatio… (full text at CIViC) PMID 23816960 · Sequist et al., 2013 · Open in CIViC	civic