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asciminib
Asciminib is a BCR-ABL1 tyrosine kinase inhibitor. It specifically targets the ABL myristoyl pocket at a location distinct from the ATP-binding domain, and inhibits the activity of both wild-type BCR-ABL and certain mutation forms. This results in inhibition of BCR-ABL1-mediated cell proliferation and enhanced apoptosis of Philadelphia chromosome positive (Ph+) blood cancers.
| T max |
2 to 3 hours |
| Time to reach steady state |
3 days |
| Effects with food |
Exposure is decreased by 62% with a high-fat meal and by 30% with a low-fat meal compared to the fasted state. |
Mainly distributed to plasma.
| PPB |
97% |
Metabolized by CYP3A4 oxidation, and UGT2B7- and UGT2B17-mediated glucuronidation.
| Feces |
80% (57% unchanged) |
| Urine |
11% (3% unchanged) |
| Half-life |
7-15 hours (terminal) |
- Chronic myeloid leukemia (Ph+ CML) in chronic phase
Refer to the product monograph for a full list and details of approved indications.
Emetogenic Potential:
The following table lists adverse effects that occurred in ≥ 10% of patients who received asciminib in a phase III clinical trial in chronic phase Ph+ CML. Severe or life-threatening adverse effects from other sources or post-marketing are also included.
| ORGAN SITE | SIDE EFFECT* (%) | ONSET** | |||
|---|---|---|---|---|---|
| Cardiovascular | Arrhythmia (7%) (severe 2%) | E | |||
| Arterial thromboembolism (3%) | E | ||||
| Cardiotoxicity (4%) (severe 3%) | E D | ||||
| Hypertension (15%) | E | ||||
| QT interval prolonged (1%) | E | ||||
| Dermatological | Rash (15%) | E | |||
| Gastrointestinal | Abdominal pain (13%) | E | |||
| Diarrhea (13%) | E | ||||
| Nausea (12%) | E | ||||
| General | Fatigue (21%) | E | |||
| Hematological | Myelosuppression ± infection, bleeding (28%) (severe 19%) (including viral reactivation) | ||||
| Hepatobiliary | ↑ Amylase / lipase (23%) (severe 13%) | E | |||
| Pancreatitis (3%) (1% grade 3) | E | ||||
| Hypersensitivity | Hypersensitivity (33%) (severe 2%) | I | |||
| Metabolic / Endocrine | Hypothyroidism (1%) | E D | |||
| Other - Dyslipidemia (6%) | E D | ||||
| Musculoskeletal | Musculoskeletal pain (22%) | E | |||
| Nervous System | Headache (19%) | E | |||
| Respiratory | Cough, dyspnea (9%) | E | |||
| Pleural effusion (1%) | E | ||||
* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare"
may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal
reports.
** I = immediate (onset in hours to days)
E = early (days to weeks)
D = delayed (weeks to months)
L = late (months to years)
The most common side effects for asciminib include hypersensitivity, myelosuppression ± infection, bleeding, ↑ amylase / lipase, musculoskeletal pain, fatigue, headache, hypertension, rash, diarrhea and nausea.
In patients with severe hypertension, the median time to first occurrence was 29 weeks (range: 0.1 to 365 weeks).
Myelosuppression was very common. In patients with severe myelosuppression, the median onset of thrombocytopenia and neutropenia was 6 weeks (range: 0.1 to 180 weeks), and 30 weeks (range: 0.4 to 207 weeks) for anemia.
Refer to protocol by which patient is being treated.
Correct electrolyte imbalances before starting treatment.
Oral: 80 mg Daily
OR
Oral: 40 mg BID
| Dose Levels | Once-daily Dosing | Twice-daily Dosing |
| 0 | 80 mg Daily | 40 mg BID |
| -1 | 40 mg Daily | 20 mg BID |
| -2 | Discontinue | Discontinue |
| Toxicity | Severity | Action |
| Thrombocytopenia and/or neutropenia |
Platelets < 50 x 109/L |
Hold until platelets ≥ 50 x 109/L and ANC ≥ 1 x 109/L. If resolved:
If recurrent, hold until platelets ≥ 50 x 109/L and ANC ≥ 1 x 109/L and restart at reduced dose. |
| Asymptomatic amylase and/or lipase elevation | > 2 x ULN |
Hold until resolved to < 1.5 x ULN. If resolved, restart at reduced dose. Discontinue if it does not resolve. Investigate for pancreatitis. Discontinue at recurrence. |
| Symptomatic amylase and/or lipase elevation | Any | Hold and investigate for pancreatitis. |
| Hypersensitivity | Grade 3 or 4 | Hold, then reduce dose or discontinue as clinically indicated |
| Other related non-hematologic toxicities | Grade 3 or 4 |
Hold until ≤ grade 1. If resolved, restart at a reduced dose. Discontinue if it does not resolve. |
No dose adjustment required.
No dose adjustment required in patients with mild, moderate or severe renal impairment not requiring dialysis (absolute GFR ≥ 15 mL/min).
Asciminib has not been studied in patients with end stage renal disease requiring dialysis.
No dose adjustment required in patients ≥ 65 years of age. No overall differences in safety or efficacy were observed between patients ≥ 65 years of age and younger patients. There is insufficient data in patients ≥ 75 years.
Gender does not have a clinically significant effect on asciminib pharmacokinetics.
Race does not have a clinically significant effect on asciminib pharmacokinetics.
Safety and efficacy have not been established.
- Asciminib should be taken orally on an empty stomach, at least 1 hour before or 2 hours after food, at around the same time(s) each day.
- If administered as twice daily, the doses should be given approximately 12 hours apart.
- When switching from 40 mg BID to 80 mg once daily, patients should start taking the first once-daily dose about 12 hours after the last twice-daily dose. Then continue at 80 mg once daily.
- When switching from 80 mg once daily to 40 mg BID, patients should start taking the first twice-daily dose about 24 hours after the last once-daily dose. Then continue at 40 mg twice daily.
- If a dose is missed:
- Once-daily regimen: if a dose is missed by > 12 hours, the missed dose should be skipped and the next dose taken as scheduled.
- Twice-daily regimen: if a dose is missed by > 6 hours, the missed dose should be skipped and the next dose taken as scheduled.
- Store in original package (20ºC to 25ºC) to protect from moisture.
- Patients who have a hypersensitivity to this drug or any of its components
- Asciminib contains lactose; carefully consider use in patients with hereditary galactose intolerance, severe lactase deficiency or glucose-galactose malabsorption.
- Cardiotoxicity occurred in patients with pre-existing cardiovascular conditions or risk factors, and/or previous exposure to multiple TKIs.
Other Drug Properties:
-
Carcinogenicity:
Unknown
Tumours observed in animals; relevance in humans unknown.
-
Phototoxicity:
Documented in animals
-
Embryotoxicity:
Documented in animals
-
Fetotoxicity:
Documented in animals
-
Abortifacient effects:
Yes
-
Teratogenicity:
Yes
-
Pregnancy:
Asciminib is not recommended for use in pregnancy. Adequate contraception should be used by patients and their partners during treatment, and for at least 1 week after the last dose.
-
Breastfeeding:
Breastfeeding is not recommended during treatment and for at least 1 week after the last dose.
-
Fertility effects:
Probable
Documented in animal studies
In vitro, asciminib is a substrate of BCRP and P-gp. It is an inhibitor of BCRP, P-gp, OATP1B1, and OATP1B3.
Co-administration of a strong CYP3A4 inhibitor, proton pump inhibitor, or P-gp inhibitor with asciminib had no clinically significant effects on asciminib exposure or Cmax.
| AGENT | EFFECT | MECHANISM | MANAGEMENT |
|---|---|---|---|
| Combined OATP1B and BCRP substrates (e.g. atorvastatin, rosuvastatin) | ↑ substrate exposure | Possible inhibition by asciminib (in vitro) | Avoid |
| Hydroxypropyl-β-cyclodextrin-containing drug formulations (e.g. itraconazole) | ↓ asciminib exposure by 40% | Possible sequestration of asciminib by hydroxypropyl-β-cyclodextrin | Avoid |
| Drugs that may prolong QT (i.e. clarithromycin, haloperidol, methadone, moxifloxacin or pimozide, etc.) | ↑ risk of QT prolongation and torsades de pointes; arrhythmia reported in clinical trials | Additive | Caution |
| CYP3A4 substrates (e.g. cyclosporine, pimozide, tacrolimus, triazolo-benzodiazepines, dihydropyridine calcium-channel blockers, certain HMG-CoA reductase inhibitors) | ↑ substrate exposure by up to 28% | Asciminib inhibits CYP3A4 | Caution with concomitant use of substrates with a narrow therapeutic index |
| Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, phenytoin or St. John’s wort) | ↓ asciminib exposure by 15% (rifampin) | ↑ metabolism of asciminib | Caution |
| CYP 2C9 substrates (e.g. warfarin, meloxicam, fluvastatin) | ↑ substrate exposure by up to 52% | Asciminib inhibits CYP2C9 | Caution with concomitant use of substrates with a narrow therapeutic index. Consider dose adjustment of CYP2C9 substrates. |
| P-glycoprotein substrates (i.e. verapamil, digoxin, dabigatran) | ↑ substrate exposure (up to 34%) | Asciminib inhibits P-gp | Caution with concomitant use of substrates with a narrow therapeutic index |
| BCRP substrates (e.g. sulfasalazine, methotrexate) | ↑ substrate exposure | Possible inhibition by asciminib (in vitro) | Caution; adjust substrate dose as recommended by its product monograph |
| OATP1B substrates (e.g. pravastatin, simvastatin) | ↑ substrate exposure | Possible inhibition by asciminib (in vitro) | Caution; adjust substrate dose as recommended by its product monograph |
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
Refer to the hepatitis B virus screening and management guideline for monitoring during and after treatment.
| Monitor Type | Monitor Frequency |
|---|---|
CBC |
Baseline, every 2 weeks for the first 3 months, then monthly thereafter, and as clinically indicated |
Amylase and lipase |
Baseline, monthly, and as clinically indicated, more frequent monitoring in patients with a history of pancreatitis |
Electrolytes |
Baseline, at each visit, and as clinically indicated |
Blood pressure |
Baseline, at each visit, and as clinically indicated |
ECG |
Baseline and as clinically indicated |
Liver function tests |
Baseline and as clinically indicated |
Renal function tests |
Baseline and as clinically indicated |
Clinical toxicity assessment for fatigue, bleeding, infection, musculoskeletal pain, hypersensitivity, thromboembolism, cardiac and GI effects |
At each visit |
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
Exceptional Access Program (EAP Website )
- asciminib - For the treatment of Philadelphia chromosome-positive chronic myeloid leukemia in chronic phase, based on criteria
Hoch M, Huth F, Sato M, et al. Pharmacokinetics of asciminib in the presence of CYP3A or P-gp inhibitors, CYP3A inducers, and acid-reducing agents. Clin Transl Sci 2022 Jul;15(7):1698-712.
Product monograph: asciminib (Scemblix). Novartis Pharmaceuticals Canada Inc., July 2024.
Prescribing information: asciminib (Scemblix). Novartis Pharmaceuticals Corp. (USA), November 2023.
Rea D, Mauro MJ, Boquimpani C, et al. A phase 3, open-label, randomized study of asciminib, a STAMP inhibitor, vs bosutinib in CML after 2 or more prior TKIs. Blood Nov 2021; 138(21): 2031-41.
July 2025 New drug monograph
Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.
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