asciminib

Strong CYP3A4 inhibitors, including clarithromycin, may ↑ levels and risk of toxicity; closely monitor patients using asciminib 200 mg twice daily.
Itraconazole (oral solution), containing hydroxypropyl-β-cyclodextrin, may ↓ levels and effectiveness; avoid concurrent use.
May ↑ levels and risk of toxicity of CYP3A4 substrates, including midazolam; closely monitor when using asciminib 40 mg twice daily or 80 mg once daily. Avoid concurrent use with asciminib 200 mg twice daily.
May ↑ levels and risk of toxicity of CYP2C9 substrates, including warfarin; avoid concurrent use with asciminib 40 mg twice daily or 80 mg once daily; if concurrent use unavoidable, ↓ dose of CYP2C9 substrate. Avoid concurrent use with asciminib 200 mg twice daily; if concurrent use unavoidable, use non-CYP2C9 substrate.
May ↑ levels and risk of toxicity of P-glycoprotein substrates.
May ↑ levels and risk of toxicity of BRCP substrates and OATP1B substrates, including atorvastatin and rosuvastatin; avoid concurrent use with atorvastatin or rosuvastatin.

Availability ⬆ ⬇

Film-coated tablets: 20 mg; 40 mg; 100 mg

Route/Dosage ⬆ ⬇

Newly Diagnosed or Previously Treated Ph+ CML in Chronic Phase

PO (Adults ): 80 mg once daily or 40 mg every 12 hr.

Ph+ CML in Chronic Phase with the T315I Mutation

PO (Adults ): 200 mg every 12 hr.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a ABL/BCR-ABL1 tyrosine kinase inhibitor, resulting in inhibition of leukemic cell lines.

Therapeutic effects:

Inhibits production of malignant cells lines with decreased proliferation of leukemic cells.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration. Absorption ↓ by food.

Distribution: Extensively distributed to tissues.

Protein Binding: 97%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme and via glucuronidation. 80% excreted in the feces (57% as unchanged drug), with 11% excreted in the urine (2.5% as unchanged drug). Also eliminated by biliary secretion by the breast cancer resistance protein (BCRP).

Half-Life: 40 mg twice daily or 80 mg once daily: 5.5 hr; 200 mg twice daily: 9 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take the medication exactly as prescribed. If patients taking once daily miss a dose by >12 hr, skip the missed dose, and take next dose as scheduled. If patients taking twice daily miss a dose by >6 hr, skip the missed dose, and take next dose as scheduled. Do not change the dose, schedule, or stop taking it unless told by an health care professional.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Instruct patient to contact a health care professional for ↑ BP and/or symptoms of hypertension.
Advise patient to report signs and symptoms of myelosuppression, pancreatic toxicity, or cardiovascular toxicity to a health care professional immediately.
Instruct the patient to discontinue asciminib and seek immediate medical attention if any signs or symptoms of a hypersensitivity reaction occur.
Rep: May cause fetal harm. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise women of reproductive potential to use effective contraception during and for 1 wk after last dose. Do not breastfeed during treatment and for 1 wk after the last dose.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

0078- Novartis Pharmaceuticals Corporation
- 0078-1091- SCEMBLIX
  - 0078-1091-20- 60 TABLET, FILM COATED in 1 BOTTLE (0078-1091-20)

0078- Novartis Pharmaceuticals Corporation
- 0078-1091- SCEMBLIX
  - 0078-1091-94- 14 TABLET, FILM COATED in 1 BOTTLE (0078-1091-94)

0078- Novartis Pharmaceuticals Corporation
- 0078-1098- SCEMBLIX
  - 0078-1098-20- 60 TABLET, FILM COATED in 1 BOTTLE (0078-1098-20)

0078- Novartis Pharmaceuticals Corporation
- 0078-1098- SCEMBLIX
  - 0078-1098-94- 14 TABLET, FILM COATED in 1 BOTTLE (0078-1098-94)

0078- Novartis Pharmaceuticals Corporation
- 0078-1196- SCEMBLIX
  - 0078-1196-20- 60 TABLET, FILM COATED in 1 BOTTLE (0078-1196-20)

17088- Novartis Pharma Stein AG
- 17088-0156-
  - 17088-0156-1- 25000 TABLET, FILM COATED in 1 DRUM (17088-0156-1)

17088- Novartis Pharma Stein AG
- 17088-0163-
  - 17088-0163-1- 25000 TABLET, FILM COATED in 1 DRUM (17088-0163-1)

44139- Novartis Pharma Schweizerhalle AG
- 44139-0104-
  - 44139-0104-7- 5 kg in 1 BAG (44139-0104-7)

54893- MSN Laboratories Private Limited
- 54893-0517-
  54893-0517-1- 13 kg in 1 DRUM (54893-0517-1)

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇