alectinib

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Severe renal impairment or end-stage renal disease;
Severe hepatic impairment (↓ dose);
Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, edema

Derm: photosensitivity, rash

EENT: blurred vision, diplopia

Endo: hyperglycemia

F and E: hypocalcemia, hypokalemia, hyponatremia, hypophosphatemia

GI: constipation, diarrhea, hyperbilirubinemia, nausea, vomiting, HEPATOTOXICITY

GU: ↑serum creatinine

Hemat: anemia, lymphopenia, BLEEDING, hemolytic anemia

Metab: ↑weight

MS: ↑creatine kinase, back pain, myalgia

Neuro: fatigue, headache

Resp: cough, dyspnea, INTERSTITIAL LUNG DISEASE (ILD), PULMONARY EMBOLISM

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Capsules: 150 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 600 mg twice daily.

Hepatic Impairment

PO (Adults ): Severe hepatic impairment: 450 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits tyrosine kinase receptors targeting ALK and RET.

Therapeutic effects:

Decreased spread of NSCLC.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 37% absorbed following oral administration; high-fat, high-calorie meals ↑ absorption.

Distribution: Extensively distributed to tissues.

Protein Binding: 99%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme to its active metabolite, M4 (also metabolized by CYP3A4). 84% excreted in feces unchanged; minimal excretion in urine.

Half-Life: Alectinib: 33 hr; M4 active metabolite: 31 hr.

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4 hr	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take alectinib as directed. If a dose is missed or vomiting occurs after taking, omit dose and take next dose at scheduled time. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Advise patient to use sunscreen and lip balm (SPF ≥50) and to wear protective clothing to prevent photosensitivity reaction.
Advise patient to notify health care professional if signs and symptoms of liver problems (feeling tired, itchy skin, feeling less hungry than usual, nausea or vomiting, yellowing of skin or whites of eyes, pain on right side of stomach, dark urine, bleeding or bruising more easily than normal), respiratory problems (trouble breathing, shortness of breath, cough, fever), bradycardia (dizziness, lightheadedness, syncope), or myalgia (unexplained muscle pain, tenderness, or weakness) occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception and avoid breastfeeding during and for at least 1 wk following therapy. Advise males with female partners of reproductive potential to use effective contraception during and for 3 mo after last dose.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

50242- Genentech, Inc.
- 50242-130- ALECENSA
  - 50242-130-01- 1 BOTTLE, PLASTIC in 1 CARTON (50242-130-01) > 240 CAPSULE in 1 BOTTLE, PLASTIC

50242- Genentech, Inc.
- 50242-130- ALECENSA
  - 50242-130-86- 1 BOTTLE, PLASTIC in 1 CARTON (50242-130-86) > 240 CAPSULE in 1 BOTTLE, PLASTIC

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Indications ⬇

Contraind./Precautions ⬆ ⬇