BYQLOVI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BYQLOVI (BYQLOVI).
BYQLOVI (revumenib) is a menin inhibitor that binds to the menin protein, blocking its interaction with mixed lineage leukemia (MLL) fusion proteins and thus inhibiting leukemogenesis.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2D6. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 95% of elimination; fecal excretion is minimal (<5%). |
| Half-life | Terminal elimination half-life is approximately 12 hours (range 10–14 hours) in patients with normal renal function; prolonged in renal impairment. |
| Protein binding | Approximately 85% bound to serum albumin. |
| Volume of Distribution | Volume of distribution is about 0.6 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is approximately 80% (range 75–85%) under fasting conditions; food may reduce absorption. |
| Onset of Action | Oral: clinical effect observed within 2–4 hours post-dose. |
| Duration of Action | Duration of action is approximately 24 hours with once-daily dosing, consistent with steady-state trough levels. |
BYQLOVI (bictegravir/emtricitabine/tenofovir alafenamide) is administered orally as a single tablet (50/200/25 mg) once daily with or without food.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | Contraindicated in patients with estimated creatinine clearance (CrCl) <30 mL/min. No dose adjustment required for CrCl ≥30 mL/min. |
| Liver impairment | Not recommended in patients with severe hepatic impairment (Child-Pugh Class C). No dose adjustment required for mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment. |
| Pediatric use | For adolescents aged ≥12 years and weighing ≥35 kg, administer one tablet (50/200/25 mg) orally once daily. Safety and efficacy not established in pediatric patients <12 years or <35 kg. |
| Geriatric use | No specific dose adjustment recommended in elderly patients. Monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BYQLOVI (BYQLOVI).
| Breastfeeding | Breastfeeding not recommended during BYQLOVI therapy due to potential for HIV-1 transmission via breast milk and unknown effects in infants. Bictegravir excretion into human milk unknown; emtricitabine: M/P ratio ~0.6; tenofovir alafenamide: M/P ratio ~0.3 (tenofovir). Limited data: low levels may be excreted. HIV-positive mothers should not breastfeed to avoid transmission. |
| Teratogenic Risk | BYQLOVI (bictegravir/emtricitabine/tenofovir alafenamide) is contraindicated in pregnancy due to risk of neural tube defects (NTDs) observed with dolutegravir-containing regimens in first trimester exposure. In animal studies, no evidence of teratogenicity at clinically relevant exposures. Human data: insufficient for risk assessment; case reports of NTDs with bictegravir insufficient to rule out. First trimester: potential for NTDs, avoid unless benefit outweighs risk. Second/third trimester: limited data, no specific fetal risks identified, but use alternative if possible. |
■ FDA Black Box Warning
No FDA boxed warning reported.
| Serious Effects |
None reported.
| Precautions | ["Differentiation syndrome, which may be life-threatening or fatal; if suspected, initiate corticosteroids and hemodynamic monitoring.","QTc interval prolongation; monitor electrolytes and electrocardiograms.","Embryo-fetal toxicity."] |
| Food/Dietary | Avoid grapefruit, grapefruit juice, Seville oranges, and starfruit as they inhibit CYP3A4 and can increase drug levels, leading to toxicity. No other known food interactions. Take with or without food, but consistent timing and fat content is recommended to maintain stable exposure. |
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| Fetal Monitoring | Monitor HIV-1 RNA and CD4+ cell count at baseline and regularly during treatment. Assess renal function (serum creatinine, estimated creatinine clearance, urine glucose and protein) at baseline and periodically. Monitor for hepatitis B virus reactivation in co-infected patients. Hepatic function monitoring in patients with underlying hepatic impairment. No specific fetal monitoring required, but standard prenatal care recommended. |
| Fertility Effects | No human studies on fertility effects. Animal studies: bictegravir and emtricitabine showed no impairment of fertility at exposures 17-37 times human exposure. Tenofovir alafenamide at >34 times human exposure reduced fertility indices in rats. Clinical significance unknown. |
| Clinical Pearls |
| BYQLOVI (bruton tyrosine kinase inhibitor) is indicated for chronic lymphocytic leukemia (CLL) and Waldenström macroglobulinemia. Monitor for atrial fibrillation, hypertension, and bleeding risk. Administer with a full glass of water and do not crush or open capsules. Dose reduction may be needed with strong CYP3A4 inhibitors. Avoid concurrent use with warfarin or other anticoagulants if possible. |
| Patient Advice | Take exactly as prescribed, with a full glass of water. · Do not open, break, or chew the capsules; swallow whole. · Avoid grapefruit, grapefruit juice, Seville oranges, and starfruit while on this medication. · Report any signs of bleeding (e.g., unusual bruising, black stools) or irregular heartbeat immediately. · Avoid activities that may cause injury due to increased bleeding risk. · Use effective contraception during treatment and for at least 1 month after the last dose. |