[Afatinib (BIBW 2992)]

N Prim1, M Fore1, B Mennecier1

  • 1Service de pneumologie, pôle de pathologie thoracique, nouvel hôpital civil, hôpitaux universitaires de Strasbourg, 1, porte de l'Hôpital, 67091 Strasbourg cedex, France.

Insights

Afatinib, an irreversible HER receptor tyrosine kinase inhibitor, shows promise for advanced solid tumors, particularly metastatic non-small cell lung cancer (NSCLC) with EGFR mutations. It received FDA and European approval in 2013 for first-line treatment.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Afatinib is an irreversible multi-target HER receptor tyrosine kinase inhibitor.
  • Investigated for advanced solid tumors, including non-small cell lung cancer (NSCLC).

Purpose of the Study:

  • To report and comment on the main results of clinical studies involving afatinib in lung cancer patients.
  • Evaluate afatinib's efficacy in advanced solid tumors, particularly NSCLC.

Main Methods:

  • Phase I, II, and III clinical studies were conducted.
  • Patient selection based on prior EGFR-TKI response or EGFR activating mutation status.
  • Afatinib administered as a single agent or in combination therapies.

Main Results:

  • Afatinib demonstrated efficacy in patients with advanced solid tumors.
  • Specific focus on metastatic NSCLC patients with EGFR mutations.
  • Received FDA approval in June 2013 and European approval in September 2013 for first-line treatment of metastatic NSCLC with EGFR mutations.

Conclusions:

  • Afatinib is an approved targeted therapy for first-line treatment of metastatic NSCLC with EGFR mutations.
  • The drug's development involved extensive clinical trials to establish its efficacy and safety profile.

Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
689
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
614
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.0K
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
816