ensartinib

Contraindicated in:

Hypersensitivity (contains tartrazine);
Severe hepatic impairment (total bilirubin >3 times upper limit of normal [ULN]);
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Aspirin hypersensitivity;
Moderate hepatic impairment (total bilirubin >1.5–≥3 times ULN);
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have ↑ risk of adverse reactions.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, dry skin, pruritus, rash, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), photosensitivity

EENT: blurred vision, diplopia, photopsia, visual impairment, vitreous floaters

Endo: hyperglycemia

F and E: hypocalcemia, hyponatremia, hypophosphatemia, hypermagnesemia, hypokalemia

GI: ↑liver enzymes, constipation, hypoalbuminemia, nausea, vomiting, ↑amylase, HEPATOTOXICITY

GU: ↑serum creatinine

Hemat: anemia, bleeding, lymphopenia

Metab: ↓appetite, hyperuricemia

MS: ↑CK, pain

Neuro: dizziness, dysgeusia, fatigue

Resp: cough, respiratory tract infection, INTERSTITIAL LUNG DISEASE (ILD)/PNEUMONITIS

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors and moderate CYP3A4 inhibitors may ↑ levels and risk of toxicity; avoid concurrent use.
Strong CYP3A4 inducers and moderate CYP3A4 inducers may ↓ levels and effectiveness; avoid concurrent use.
P-glycoprotein inhibitors may ↑ levels and risk of toxicity; avoid concurrent use.

Availability ⬆ ⬇

Capsules: 25 mg; 100 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 225 mg once daily; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits ALK as well as MET and ROS1, resulting in antitumor activity.

Therapeutic effects:

Improved progression-free survival.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption following oral administration unknown.

Distribution: Extensively distributed to tissues.

Protein Binding: 91.6%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme; 91% excreted in feces (38% as unchanged drug); 10% excreted in urine (4% as unchanged drug).

Half-Life: 30 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy. If a dose is missed, take the missed dose as soon as possible unless the next dose is due within 12 hr. Do not take two doses on same day. If vomiting occurs after taking a dose, do not take an additional dose and take the next dose at its scheduled time.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
Advise patient of the signs/symptoms of severe adverse reactions such as hepatotoxicity and ILD/pneumonitis. If symptoms occur, notify health care provider immediately.
Inform patient of dermatologic adverse reactions. Advise to limit direct sun exposure during treatment and for >1 wk after discontinuation.
Advise patient to report any unexplained muscle pain, tenderness, or weakness.
Inform patient of the risks of new or worsening hyperglycemia during treatment and the need to periodically monitor glucose levels. Advise patients with diabetes mellitus or glucose intolerance that antihyperglycemic medications may need to be adjusted during treatment.
Advise patient that this product contains FD&C Yellow No. 5 (tartrazine), which may cause allergic-type or asthma-type reactions in certain susceptible persons (e.g., patients who also have aspirin hypersensitivity). Advise patient to seek immediate medical attention if symptoms of an allergic reaction occur.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected. Advise women not to breastfeed during treatment and for 1 wk after last dose. Advise women of reproductive potential and men with female partners of reproductive potential to use effective contraception during treatment and for 1 wk after last dose.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

83076- Xcovery Holdings, Inc.
- 83076-1025- ENSACOVE
  - 83076-1025-3- 30 CAPSULE in 1 BOTTLE (83076-1025-3)

83076- Xcovery Holdings, Inc.
- 83076-1100- ENSACOVE
  - 83076-1100-6- 60 CAPSULE in 1 BOTTLE (83076-1100-6)

84637- Betta Pharmaceuticals Co., Ltd.-Site C
- 84637-4023-
  - 84637-4023-1- 13 kg in 1 BAG (84637-4023-1)

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Indications ⬇

Contraind./Precautions ⬆ ⬇