ALYQ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALYQ (ALYQ).
ALYQ (alectinib) is a selective and potent anaplastic lymphoma kinase (ALK) inhibitor. It inhibits ALK autophosphorylation and downstream signaling pathways (STAT3, PI3K/AKT, MAPK), leading to apoptosis in ALK-positive tumor cells.
| Metabolism | Metabolized primarily by CYP3A4; also a substrate of P-glycoprotein. The major active metabolite (M4) is formed by CYP3A4 and contributes to clinical activity. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 70-80%) and biliary/fecal elimination (20-30%) following intravenous administration. |
| Half-life | Terminal elimination half-life is approximately 6-8 hours in adults with normal renal function; prolonged in renal impairment. |
| Protein binding | Approximately 30-40% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.6-1.0 L/kg, indicating distribution into total body water and tissues. |
| Bioavailability | Oral bioavailability is approximately 80-90%. |
| Onset of Action | Intravenous: rapid onset within minutes. Oral: onset within 1-2 hours. |
| Duration of Action | Duration of antimicrobial effect is approximately 12-24 hours depending on dose and pathogen susceptibility. |
| Molecular Weight | 367.46 |
Intravenous: 400 mg on Day 1, then 200 mg daily for 4 days; total 5 doses per cycle.
| Dosage form | TABLET |
| Renal impairment | GFR ≥30 mL/min: no adjustment; GFR <30 mL/min: reduce dose to 300 mg on Day 1, then 150 mg daily for 4 days; not recommended in dialysis. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: avoid use. |
| Pediatric use | Not established; safety and efficacy in pediatric patients not determined. |
| Geriatric use | No specific dose adjustment; monitor renal function and adjust per renal criteria. |
| 1st trimester | Limited human data; animal studies have shown teratogenic effects at high doses. Use only if potential benefit justifies risk. |
| 2nd trimester | No adequate human studies; consider maternal and fetal risks. |
| 3rd trimester | May cause fetal harm based on mechanism; avoid use near term. |
Clinical note
Comprehensive clinical and safety monograph for ALYQ (ALYQ).
| Placental transfer | Evidence of placental transfer in animal studies; likely crosses human placenta due to molecular size. |
| Breastfeeding | Unknown if excreted in human milk; due to potential for serious adverse reactions in nursing infants, discontinue drug or nursing. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to ALYQ or any componentSevere hepatic impairment
| Precautions | Hepatotoxicity (elevated AST/ALT, bilirubin; monitor liver function), Interstitial lung disease/pneumonitis (monitor for pulmonary symptoms), Severe myalgia or creatine phosphokinase (CPK) elevation (monitor CPK levels), Bradycardia (monitor heart rate and blood pressure), Severe gastrointestinal adverse reactions (diarrhea, nausea, vomiting), Embryo-fetal toxicity (can cause fetal harm; advise contraception) |
| Food/Dietary | High-fat meals significantly reduce absorption of aliskiren. Administer with a low-fat meal or on an empty stomach, consistently. Avoid grapefruit juice as it may alter drug levels. Avoid potassium-rich foods in large amounts if taking with other drugs that raise potassium. |
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| L4 - Possibly Hazardous |
| Teratogenic Risk | ALYQ is contraindicated in pregnancy. First trimester: High risk of major congenital malformations (neural tube defects, cardiovascular anomalies). Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, and neonatal renal impairment. Pregnancy must be excluded before initiation and effective contraception used during therapy and for 1 month after discontinuation. |
| Fetal Monitoring | Baseline and monthly renal function (serum creatinine, BUN), complete blood count with differential, urinalysis, and fetal ultrasound every 4 weeks from week 20 to assess growth and amniotic fluid volume. Monitor for maternal hypertension and proteinuria. |
| Fertility Effects | Reversible impairment of spermatogenesis in males (decreased sperm count and motility). In females, potential for ovarian suppression and menstrual irregularities. Effects on fertility are generally reversible upon discontinuation. |
| Clinical Pearls | ALYQ (aliskiren) is a direct renin inhibitor used for hypertension. It should not be used with ACE inhibitors or ARBs due to increased risk of hypotension, hyperkalemia, and renal impairment. Avoid in pregnancy and severe renal impairment (eGFR <30 mL/min). Monitor serum potassium and renal function regularly. Administer with a low-fat meal or on an empty stomach to avoid reduced absorption. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily. · Do not take with high-fat meals as they decrease absorption. · Avoid potassium supplements and salt substitutes containing potassium. · Seek immediate medical attention if you experience signs of allergic reaction (hives, difficulty breathing, swelling of face/lips/tongue/throat). · Tell your doctor if you become pregnant or plan to become pregnant; this drug can cause fetal harm. · You may experience dizziness or lightheadedness; avoid driving until you know how this medication affects you. |