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Screen for hepatitis B virus in all cancer patients starting systemic treatment. Find out more about hepatitis B virus screening and management.

Drug Formulary information is intended for use by healthcare professionals. It is not intended to be medical advice. Some of the information, including information about funding for cancer drugs, does not apply to all patients. Cancer treatment plans are unique to each patient. If you are a patient, please speak with your healthcare team to understand how this information applies to you.


( al-EK-ti-nib )
Exceptional Access Program
  • alectinib - Treatment of non-small cell lung cancer, according to specific criteria
Other Name(s): Alecensaro®
Appearance: White capsule
A - Drug Name


COMMON TRADE NAME(S):   Alecensaro®

B - Mechanism of Action and Pharmacokinetics

Alectinib is a highly selective and potent ALK and RET (Rearranged during Transfection) tyrosine kinase inhibitor. It inhibits ALK phosphorylation and ALK-mediated downstream signalling pathways (STAT 3 and PI3K/AKT) and induces apoptosis. Alectinib has shown activity against mutant forms of the ALK enzyme, including mutations responsible for resistance to crizotinib.


Rapidly absorbed; Tmax approx. 4 to 6 hours after oral administration


37% (under fed conditions)

T max

~4-6 hours

Time to reach steady state

7 days

Effects with food

Exposure increased 3-fold after a high-fat, high-calorie meal vs fasting


Extensive distribution into tissues


> 99% (human plasma proteins)

Cross blood brain barrier?

Yes (alectinib). CNS penetration of M4 metabolite has not been studied.

Main enzymes involved


Active metabolites

Yes (M4 has shown similar in vitro potency and activity to alectinib)


98% (84% alectinib and 6% M4)




~33 hours (alectinib) and ~31 hours (M4)

C - Indications and Status
Health Canada Approvals:

  • Non-small cell lung cancer (NSCLC)

Refer to the product monograph for a full list and details of approved indications.

D - Adverse Effects

Emetogenic Potential:  

Low – No routine prophylaxis; PRN recommended

The following table lists adverse effects that occurred in ≥ 2% of patients treated with alectinib in the Phase III clinical trial in first-line NSCLC. Severe adverse effects from other studies or post-marketing are also included.

Cardiovascular Atrioventricular block (rare) E  D
Bradycardia (11%) E
QT interval prolonged (rare) E  D
Venous thromboembolism (rare) E
Dermatological Dry skin (4%) E
Photosensitivity (5%) E  D
Rash (15%) E
Gastrointestinal Constipation (34%) E
Diarrhea (12%) E
GI perforation (rare) E  D
Mucositis (3%) E
Nausea, vomiting (14%) E
General Edema (22%) E
Fatigue (26%) E  D
Hematological Anemia (20%) (5% severe) E  D
Hemolytic anemia (rare) E
Hepatobiliary Drug-induced liver injury (rare) E
↑ LFTs (21%) (5% severe) E
Musculoskeletal Musculoskeletal pain (23%) E
↑CPK (5%) (3% severe) E
Nervous System Dizziness (8%) E
Dysgeusia (3%) E
Ophthalmic Visual disorders (5%) E
Renal Creatinine increased (8%) (1% severe) E
Nephrotoxicity (3%) E
Respiratory Other - Pneumonitis / eosinophilic pneumonia (rare) E  D

* "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 alectinib include constipation, fatigue, musculoskeletal pain, edema, ↑ LFTs, anemia, rash, nausea, vomiting, diarrhea and bradycardia.

Bradycardia correlates with plasma levels and is reversible. Patients should be informed about symptoms of bradycardia and advised to report these to the health care team.

Hepatotoxicity usually occurs during the first 3 months of therapy and is usually transient and reversible.

Myalgia and elevations of creatinine phosphokinase (CPK) have been observed and usually present early.

Hemolytic anemia has been reported during post-marketing. If suspected, initiate appropriate laboratory testing.

E - Dosing

Refer to protocol by which patient is being treated.

Screen for hepatitis B virus in all cancer patients starting systemic treatment. Refer to the hepatitis B virus screening and management guideline.

Patients must have documented ALK-positive status, based on a validated ALK assay, prior to starting treatment with alectinib.

Patients must avoid sun exposure while on treatment and for at least 7 days after the last dose, and must use UVA/B sunscreen and lip balm (at least SPF 50).


Oral: 600 mg BID

Dosage with Toxicity:

Dose level Dose (mg) BID
Starting Dose 600
-1 450
-2 300
-3 Discontinue




GI perforation


ILD/pneumonitis of any Grade

Hold; if confirmed, discontinue.

Grade 3 Renal Impairment

Hold until serum creatinine recovers to baseline or ≤ Grade 1, then resume at 1 dose level ↓.

Grade 4 Renal Impairment


≥ Grade 3 ALT or AST elevation (> 5 x ULN)
Total bilirubin ≤ 2 x ULN

Hold until recovery to baseline or ≤ Grade 1;

Resume at 1 dose level ↓.

≥ Grade 2 ALT or AST elevation (> 3 x ULN)
Total bilirubin ≥ 2 x ULN
(in absence of cholestasis or hemolysis)


Grade 2 to 3 Bradycardia (HR < 60 bpm) (symptomatic)

Hold until recovery to ≤ Grade 1 (asymptomatic) bradycardia or HR of ≥ 60 bpm.

Evaluate concomitant medications; if contributing, discontinue or reduce dose of concomitant drug. Resume at previous dose.

If no concomitant medication contributing, or contributing medication not stopped/reduced: resume at 1 dose level ↓

Grade 4 Bradycardia (HR < 60 bpm)
(life-threatening consequences, urgent intervention required)

Discontinue if no contributing concomitant medication.

If contributing concomitant medication is discontinued or reduced: Hold until recovery to ≤ Grade 1 (asymptomatic) bradycardia or HR of ≥ 60 bpm, with frequent monitoring. Resume at 1 dose level ↓.

If recurs: discontinue.

CPK elevation > 5 x ULN

Hold until recovery to baseline or ≤ 2.5 x ULN; resume at same dose.

CPK elevation > 10 x ULN
2nd Occurrence of CPK elevation > 5 x ULN

Hold until recovery to baseline or ≤ 2.5 x ULN; resume at 1 dose level ↓.

Hemolytic anemia with hemoglobin of < 100 g/L
(≥ Grade 2)
Hold until recovery, then resume at 1 dose level ↓.

Dosage with Hepatic Impairment:

Pre-existing Hepatic impairment Alectinib Dose

Mild or Moderate

No dose adjustment required.


450 mg twice daily.

Dosage with Renal Impairment:

Renal Impairment Alectinib Dose

Mild or Moderate
(CrCl ≥ 30 mL/min)

No dose adjustment required
(CrCl < 30 mL/min)
Has not been studied

Dosage in the elderly:

No dose adjustment required. Fatal adverse events and adverse events leading to treatment withdrawal were more common in patients 65 years or older compared to younger patients.


Safety and efficacy have not been established. Non-clinical studies showed effects on bone and dentition.

F - Administration Guidelines


  • Alectinib should be taken with food (fasted state decreases exposure three fold).
  • Capsules should not be opened or dissolved.
  • If a dose is missed the next dose should be taken at the next scheduled time.
  • If vomiting occurs, a repeat dose should not be taken; the next dose should be taken at the next scheduled time.
  • Avoid grapefruit, grapefruit juice, products with grapefruit extract, star fruit, Seville oranges, pomegranate, and other similar fruits that inhibit CYP3A4 during alectinib treatment due to risk for increased toxicity.
  • Store between 15-30ºC in the original package.
G - Special Precautions

  • Patients who have a hypersensitivity to this drug or any of its components 

Other Warnings/Precautions:

  • Use with caution in patients who are at risk for gastrointestinal perforation (e.g., concomitant use of medications with GI perforation risk, history of diverticulitis, metastases to the GI tract).
  • Use with caution in patients with hepatic impairment or renal impairment.
  • Use with caution in patients who have bradycardia at baseline (< 60 bpm), a history of syncope or arrhythmia, sick sinus syndrome, sinoatrial block, AV block, ischemic heart disease, CHF or who are on medications that lower HR.
  • Vision disorders, asthenia, fatigue and dizziness have been reported.  Patients with these symptoms should use caution when driving or operating machines.
  • Contains lactose; carefully consider use in patients with hereditary galactose intolerance, severe lactase deficiency or glucose-galactose malabsorption.

Other Drug Properties:

  • Carcinogenicity: Unknown
  • Phototoxicity: Likely

Pregnancy and Lactation:
  • Mutagenicity: Probable
  • Abortifacient effects: Yes
  • Embryotoxicity: Yes
  • Fetotoxicity: Yes

    Alectinib is not recommended for use in pregnancy. Adequate contraception should be used by both sexes during treatment, and for at least 3 months after the last dose.

  • Excretion into breast milk: Unknown

    Breastfeeding is not recommended.

  • Fertility effects: Unknown
H - Interactions

  • CYP3A4 is the primary enzyme responsible for metabolism of alectinib and M4 (active metabolite).  M4 has shown similar in vitro potency and activity to alectinib against ALK. 
  • Alectinib is not a substrate of P-gp while M4 is a substrate of P-gp
  • Alectinib and M4 are not substrates of BCRP or OATP 1B1/B3
  • Medications that increase gastric pH do not appear to have an effect on alectinib or M4 exposure.
  • Neither alectinib nor M4 are inhibitors of CYP1A2, 2B6, 2C9, 2C19, or 2D6.  Alectinib is a weak inhibitor of 3A4 and 2B6.
  • No dose adjustment is necessary with CYP3A4 substrates.


Strong CYP3A inducers (i.e. phenytoin, rifampin, carbamazepine, phenobarbital, St. John’s Wort, etc.) ↓ alectinib exposure and ↑ M4 exposure ↑ metabolism of alectinib Caution; monitor closely
Strong CYP3A inhibitors (i.e. ketoconazole, clarithromycin, ritonavir, fruit or juice from grapefruit, Seville oranges or starfruit) ↑ alectinib exposure and ↓ M4 exposure ↓ metabolism of alectinib Caution; monitor closely
CYP 2C8 substrates (i.e. paclitaxel, sorafenib, amiodarone) ↑ substrate concentration and/or toxicity (in vitro) ↓ metabolism of substrate Caution; monitor closely
BCRP substrates (i.e. topotecan) ↑ substrate concentration and/or toxicity (in vitro) ↓ metabolism of substrate Caution with drugs with narrow therapeutic index
P-glycoprotein substrates (i.e. verapamil, digoxin, morphine, ondansetron) ↑ substrate concentration and/or toxicity (in vitro) ↓ metabolism of substrate Caution with drugs with narrow therapeutic index
Drugs that lower heart rate (e.g. alpha2-adrenoceptor agonists, beta blockers, non-dihydropyridine Ca channel blockers, digoxin, cholinesterase inhibitors, sphingosine-1 phosphate receptor modulators) ↑ risk of bradycardia Additive Avoid if possible; if not possible, monitor closely
I - Recommended Clinical Monitoring

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.

Recommended Clinical Monitoring

Monitor Type Monitor Frequency

Liver function tests

Baseline, every 2 weeks during the first 3 months of treatment, then at each visit or as clinically indicated; more frequent with abnormal LFTs.

Blood CPK levels

Every 2 weeks for the first month, and as clinically indicated

Renal function tests

Baseline, at each visit, and as clinically indicated

Electrolytes, including serum calcium and potassium

Baseline, at each visit, and as clinically indicated

Blood pressure and heart rate

Baseline, at each visit, and as clinically indicated.


Baseline and as required to evaluate QTc, AV block.


Baseline and as clinically indicated, or if hemolytic anemia suspected

Clinical toxicity assessment for photosensitivity, rash, edema, fatigue, myalgia, dizziness, headache, visual disorders, respiratory and GI effects

At each visit

Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version

J - Supplementary Public Funding

Exceptional Access Program (EAP Website)

  • alectinib - Treatment of non-small cell lung cancer, according to specific criteria

K - References

Ou SI, Ahn JS, De Petris L, et al: Alectinib in Crizotinib-Refractory ALK-Rearranged Non-Small-Cell Lung Cancer: A Phase II Global Study. J Clin Oncol, 2015.

Product monograph: Alectinib (Alecensaro). Hoffmann-La Roche Limited. May 9, 2022.

Shaw AT, Gandhi L, Gadgeel S, et al: Alectinib in ALK-positive, crizotinib-resistant, non-small-cell lung cancer: a single-group, multicentre, phase 2 trial. Lancet Oncol 17:234-42, 2016

March 2023 Updated indications, adverse effects, dosing, special precautions, and monitoring sections

L - Disclaimer

Refer to the New Drug Funding Program or Ontario Public Drug Programs websites for the most up-to-date public funding information.

The information set out in the drug monographs, regimen monographs, appendices and symptom management information (for health professionals) contained in the Drug Formulary (the "Formulary") is intended for healthcare providers and is to be used for informational purposes only. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects of a particular drug, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for a given condition. The information in the Formulary is not intended to constitute or be a substitute for medical advice and should not be relied upon in any such regard. All uses of the Formulary are subject to clinical judgment and actual prescribing patterns may not follow the information provided in the Formulary.

The format and content of the drug monographs, regimen monographs, appendices and symptom management information contained in the Formulary will change as they are reviewed and revised on a periodic basis. The date of last revision will be visible on each page of the monograph and regimen. Since standards of usage are constantly evolving, it is advised that the Formulary not be used as the sole source of information. It is strongly recommended that original references or product monograph be consulted prior to using a chemotherapy regimen for the first time.

Some Formulary documents, such as the medication information sheets, regimen information sheets and symptom management information (for patients), are intended for patients. Patients should always consult with their healthcare provider if they have questions regarding any information set out in the Formulary documents.

While care has been taken in the preparation of the information contained in the Formulary, such information is provided on an “as-is” basis, without any representation, warranty, or condition, whether express, or implied, statutory or otherwise, as to the information’s quality, accuracy, currency, completeness, or reliability.

CCO and the Formulary’s content providers shall have no liability, whether direct, indirect, consequential, contingent, special, or incidental, related to or arising from the information in the Formulary or its use thereof, whether based on breach of contract or tort (including negligence), and even if advised of the possibility thereof. Anyone using the information in the Formulary does so at his or her own risk, and by using such information, agrees to indemnify CCO and its content providers from any and all liability, loss, damages, costs and expenses (including legal fees and expenses) arising from such person’s use of the information in the Formulary.