Asciminib

SCEMBLIX

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Pronunciation: as-KIM-i-nib (SEM-blix)

Asciminib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Asciminib ballicule

What it isAllosteric BCR-ABL1 inhibitor binding the myristoyl pocket rather than the ATP site; chronic myeloid leukemia.

Why this oneIts distinct binding site can retain activity after ATP-site inhibitors fail, including against T315I disease.

What limits itMyelosuppression, pancreatic-enzyme elevation or pancreatitis, hypertension, and arterial events require monitoring.

Asciminib molecular structure (skeletal formula) — Molecular structure: Asciminib

FDA label

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FDA dosing	Population	Start	Target	Max
Ph+ CML in chronic phase (newly diagnosed or previously treated)	Adults	80 mg QD or 40 mg BID (~12 h apart)	80 mg QD or 40 mg BID	80 mg/day
Ph+ CML-CP with T315I mutation	Adults	200 mg BID (~12 h apart)	200 mg BID	400 mg/day

Renal No adjustment needed (mild-severe, eGFR 15-89, not requiring dialysis)

Hepatic No adjustment needed (mild-severe)

Dose-reduce for adverse reactions: CML-CP 40 mg QD or 20 mg BID; T315I 160 mg BID; discontinue if not tolerated

Instructions

Take without food; avoid food >=2 h before and 1 h after each dose
Swallow tablets whole; do not break, crush, or chew
Missed dose: skip if >~12 h late (QD regimen) or >~6 h late (BID regimens); take next dose as scheduled

Available strengths

tab 20, 40, 100 mg

Cautions

Myelosuppression — CBC q2wk for first 3 months, then monthly; manage by interruption/dose reduction
Pancreatic toxicity — monitor lipase/amylase monthly; evaluate for pancreatitis if elevation with abdominal symptoms
Hypertension (18%) — monitor BP; interrupt/reduce/stop if not medically controlled
Hypersensitivity (rash, edema, bronchospasm)
Cardiovascular toxicity (ischemic, thromboembolic, cardiac failure, arrhythmia incl. QTc prolongation) — monitor patients with CV risk factors
Embryo-fetal toxicity — verify pregnancy status; effective contraception during and 1 wk after

Adverse reactions

Musculoskeletal pain
Rash
Fatigue
Upper respiratory tract infection
Headache
Abdominal pain
Arthralgia
Diarrhea
Labs: decreased lymphocytes/leukocytes/platelets/neutrophils/hemoglobin; increased lipase, cholesterol, triglycerides, uric acid, ALT/AST/ALP, CK, amylase

Pregnancy Can cause fetal harm (animal malformations at <=human exposure); verify pregnancy status before starting; contraception during and 1 wk after last dose

Lactation Do not breastfeed during treatment and for 1 week after last dose

Cost

Asciminib (SCEMBLIX)

Strength		#/mo	CostPlus
20 mg	tab	30 qd	not offered
40 mg	tab	30 qd	not offered
100 mg	tab	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Asciminib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2040 est.

NO BOXED WARNINGS

Principal riskNo FDA boxed warning.

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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