Ensartinib

ENSACOVE is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC)as detected by an FDA-approved test who have not previously received an ALK-inhibitor. ENSACOVE is a kinase inhibitor indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test who have not previously received an ALK-inhibitor.

Ensartinib is a kinase inhibitor of anaplastic lymphoma kinase (ALK) and inhibits other kinases including MET and ROS1. In vitro, ensartinib inhibited phosphorylation of ALK and its downstream signaling proteins AKT, ERK, and S6, thereby blocking ALK-mediated signaling pathways and inhibiting proliferation in cell lines harboring ALK fusions and mutations. In vivo, ensartinib showed anti-tumor activity in a mouse xenograft model of human NSCLC harboring an ALK fusion.

Select patients with ALK-positive locally advanced or metastatic NSCLC for treatment with ENSACOVE. Prior to initiating ENSACOVE, evaluate liver function tests and fasting blood glucose. Recommended dosage: 225 mg orally once daily with or without food until disease progression or unacceptable toxicity.

ENSACOVE is contraindicated in patients who have experienced a severe hypersensitivity reaction to ENSACOVE, FD&C Yellow No. 5 (tartrazine), or to any of its components. Hypersensitivity reaction to ENSACOVE, FD&C Yellow No. 5 (tartrazine), or to any of its components.

Interstitial Lung Disease (ILD)/Pneumonitis: Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis. Permanently discontinue in patients with ILD/pneumonitis. Hepatotoxicity: Monitor liver function tests during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. Dermatologic Adverse Reaction: Monitor for dermatologic adverse reactions during treatment with ENSACOVE. Bradycardia: Monitor heart rate regularly during treatment with ENSACOVE. Hyperglycemia: Monitor serum glucose periodically during treatment with ENSACOVE. Visual Disturbances: Advise patients to report visual symptoms during treatment with ENSACOVE. Withhold ENSACOVE and obtain ophthalmologic evaluation, then reduce the dose or permanently discontinue ENSACOVE.

The following clinically significant adverse reactions are described elsewhere in the labeling: Interstitial Lung Disease/Pneumonitis Hepatoxicity Dermatologic Adverse Reactions Bradycardia Hyperglycemia Visual Disturbances Increased Creatine Phosphokinase Hyperuricemia FD&C Yellow No. 5 (Tartrazine) Most common adverse reactions (incidence ≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia. Most common Grade 3-4 laboratory abnormality (incidence ≥2%) were increased uric acid, decreased lymphocytes, increased alanine aminotransferase, decreased phosphate, increased gamma glutamyl transferase, increased magnesium, increased amylase, decreased sodium, increased glucose, decreased hemoglobin, increased bilirubin, decreased potassium, and increased creatine phosphokinase.

Moderate or Strong CYP3A Inhibitors: Avoid concomitant use with ENSACOVE. Moderate or Strong CYP3A Inducers: Avoid concomitant use with ENSACOVE. P-gp Inhibitor: Avoid concomitant use with ENSACOVE.

Store at controlled room temperature 20ºC to 25ºC (68ºF to 77ºF), excursions permitted to 15ºC to 30ºC (59ºF to 86ºF). Store and dispense in the original bottle with desiccant to protect from moisture.