Ensartinib

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.

• 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 [see Dosage and Administration ( 2.1 )] 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.ICD-10: C34.90, C85.90

• 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 [see Warnings and Precautions ( 5.10 )] .contraindicated

Select patients with ALK-positive locally advanced or metastatic NSCLC for treatment with ENSACOVE. ( 2.1 ) Prior to initiating ENSACOVE, evaluate liver function tests and fasting blood glucose. ( 2.2 ) Recommended dosage: 225 mg orally once daily with or without food until disease progression or unacceptable toxicity. ( 2.3 ) 2.1 Patient Selection Select patients for the treatment of locally advanced or metastatic NSCLC with ENSACOVE based on the presence of ALK rearrangement(s) in tumor specimens [see Clinical Studies ( 14.1 )] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics . 2.2 Recommended Testing and Advice Prior to Initiating ENSACOVE Prior to initiating ENSACOVE, evaluate liver function tests [see Warnings and Precautions ( 5.2 )] and fasting blood glucose [see Warnings and Precautions ( 5.5 )]. 2.3 Recommended Dosage The recommended dosage of ENSACOVE is 225 mg orally once daily, with or without food [see Clinical Pharmacology ( 12.3 )] , until disease progression or unacceptable toxicity. Swallow capsules whole, do not crush or chew. Do not open or dissolve the contents of the capsule. Take ENSACOVE at the same time each day. Missed dose If a dose is missed, then take the missed dose as soon as possible unless the next dose is due within 12 hours. Do not take 2 doses on the same day. Vomiting If vomiting occurs after taking a dose, do not take an additional dose and take the next dose at its scheduled time.

Interstitial Lung Disease (ILD)/Pneumonitis : Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis. Permanently discontinue in patients with ILD/pneumonitis. ( 5.1 ) Hepatotoxicity : Monitor liver function tests during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. (5.2 ) Dermatologic Adverse Reaction : Monitor for dermatologic adverse reactions during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.3 ) Bradycardia : Monitor heart rate regularly during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.4 ) Hyperglycemia : Monitor serum glucose periodically during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.5 ) 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. (5.6) Increased Creatine Phosphokinase (CPK) : Monitor CPK periodically during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.7 ) Hyperuricemia : Monitor uric acid periodically during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.8 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.

The following clinically significant adverse reactions are described elsewhere in the labeling: Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions ( 5.1 )] Hepatoxicity [see Warnings and Precautions ( 5.2 )] Dermatologic Adverse Reactions [see Warnings and Precautions ( 5.3 )] Bradycardia [see Warnings and Precautions ( 5.4 )] Hyperglycemia [see Warnings and Precautions ( 5.5 )] Visual Disturbances [see Warnings and Precautions ( 5.6 )] Increased Creatine Phosphokinase [see Warnings and Precautions ( 5.7 )] Hyperuricemia [see Warnings and Precautions ( 5.8 )] FD&C Yellow No. 5 (Tartrazine) [see Warnings and Precautions ( 5.10 ) ] Most common adverse reactions (incidence ≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia. ( 6.1 ) 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. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Xcovery Holdings, Inc. at (866) 367-2268 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Lactation : Advise not to breastfeed. ( 8.2 ) Severe Hepatic Impairment: Avoid use of ENSACOVE in patients with severe hepatic impairment. (8.6 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , ENSACOVE can cause fetal harm when administered to a pregnant woman. There are no available data on the use of ENSACOVE in pregnant women to inform a drug-associated risk. Oral administration of ensartinib to pregnant rats during the period of organogenesis caused adverse developmental outcomes, including embryo-fetal mortality, alterations to growth, and structural abnormalities. Adverse embryo-fetal findings were seen at maternal exposures approximately equivalent to the human exposure at the recommended dose of 225 mg/day based on AUC ( see Data ). Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study, pregnant rats received 20, 40, or 80 mg/kg/day of ensartinib during the period of organogenesis (gestation day 6 to 17).

Metabolism

Ensartinib mean (coefficient of variation [CV%]) maximum concentration (Cmax) is 292 ng/mL (60%), and the area under the concentration-time curve (AUC0–24h) is 4,920 ng·h /ml (62%) at the approved recommended dosage. Ensartinib steady state is reached within 15 days with a mean accumulation ratio of 2.7.

• Dec 18, 2024NDANDA218171Xcovery

1. 1Drug Ineffective517%
2. 2Rash517%
3. 3Disease Progression414%
4. 4Constipation310%
5. 5Oedema310%
6. 6Pruritus310%
7. 7Alanine Aminotransferase Increased26.9%
8. 8Aspartate Aminotransferase Increased26.9%
9. 9Diarrhoea26.9%
10. 10Drug Resistance26.9%
11. 11Fatigue26.9%
12. 12Pleural Effusion26.9%
13. 13Rash Pruritic26.9%
14. 14Adrenal Insufficiency13.4%
15. 15Adverse Drug Reaction13.4%

The 10 most recently updated of 38 ClinicalTrials.gov registrations naming Ensartinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 1,377 enrolled · National Cancer Institute (NCI)
  NCT03155620updated 2026-06-01
• Ensartinib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With ALK or ROS1 Genomic Alterations (A Pediatric MATCH Treatment Trial)
  Active not recruiting · Phase 2 · Interventional · 13 enrolled · National Cancer Institute (NCI)
  NCT03213652updated 2026-05-27
• Treating Patients With Melanoma and ALK Alterations With Ensartinib
  Active not recruiting · Phase 2 · Interventional · 18 enrolled · Memorial Sloan Kettering Cancer Center
  NCT03420508updated 2026-05-13
• Ensartinib in Combination With Bevacizumab in ALK-positive NSCLC Patients With TP53 Mutation
  Active not recruiting · Phase 2 · Interventional · 47 enrolled · Sun Yat-sen University
  NCT05491811updated 2026-05-04
• Phase 1/2 Study of X-396, an Oral ALK Inhibitor, in Patients With ALK-positive Non-Small Cell Lung Cancer
  Completed · Phase 1 · Phase 2 · Interventional · 131 enrolled · Xcovery Holdings, Inc.
  NCT01625234updated 2026-04-30
• Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer
  Terminated · Phase 2 · Interventional · 10 enrolled · National Cancer Institute (NCI)
  NCT03737994updated 2026-04-23
• Neoadjuvant Umbrella Trial for Patients With Unresectable Stage III NSCLC Harboring Rare Mutations.
  Recruiting · Phase 2 · Interventional · 120 enrolled · Sun Yat-sen University
  NCT06563999updated 2026-04-21
• Neoadjuvant Therapy With Ensartinib Combined With Chemotherapy for ALK-positive Non - Small Cell Lung Cancer (NSCLC)
  Recruiting · Phase 1 · Phase 2 · Interventional · 20 enrolled · Tang-Du Hospital
  NCT07354061updated 2026-04-01
• Study of MCLA-129 in Combination With Ensartinib in Patients With Advanced Solid Tumors.
  Recruiting · Phase 1 · Phase 2 · Interventional · 164 enrolled · Betta Pharmaceuticals Co., Ltd.
  NCT07448116updated 2026-03-04
• Ensartinib, Carboplatin, Pemetrexed and Bevacizumab for the Treatment of Stage IIIC or IV or Recurrent ALK-Positive Non-small Cell Lung Cancer
  Active not recruiting · Phase 1 · Interventional · 12 enrolled · M.D. Anderson Cancer Center
  NCT04837716updated 2026-02-19

Frequently asked questions

How does Ensartinib work?

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.

What is Ensartinib used for?

According to FDA labeling, Ensartinib carries indications including: 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 [see Dosage and Administration ( 2.1 )] 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ensartinib?

Ensartinib is classified as Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Ensartinib?

Ensartinib is marketed under brand names including Ensacove.

What are the contraindications for Ensartinib?

Ensartinib labeling lists contraindications including: 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 [see Warnings and Precautions ( 5.10 )] .. Always consult the full prescribing information and a clinician.