BOSAYA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for BOSAYA (BOSAYA).

How it works

Bosaya is an endothelin receptor antagonist that selectively inhibits endothelin-1 (ET-1) from binding to ETA receptors, reducing pulmonary vascular resistance and pulmonary arterial pressure.

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 (CYP) enzymes, specifically CYP3A4 and CYP2C9, with minor contributions from CYP2C19 and CYP2D6.
Excretion	BOSAYA is primarily eliminated via hepatic metabolism with minimal renal excretion. Approximately 1% of the dose is excreted unchanged in urine, while the majority of metabolites are excreted in feces (70-80%) via biliary elimination, with less than 20% recovered in urine as metabolites.
Half-life	The terminal elimination half-life is approximately 11-14 hours in adults with normal hepatic function. This supports once-daily dosing, though dose adjustment may be needed in hepatic impairment.
Protein binding	BOSAYA is highly protein-bound (>99%), primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	The apparent volume of distribution is approximately 0.5-0.7 L/kg, indicating extensive tissue distribution, with high concentrations found in liver and kidneys.
Bioavailability	Oral bioavailability is approximately 60-80% due to first-pass hepatic metabolism. Food does not significantly affect absorption.
Onset of Action	Oral administration: Onset of therapeutic effect occurs within 2-4 hours after dosing, with maximal antihypertensive effect seen within 2-4 weeks of continuous therapy.
Duration of Action	The duration of action supports once-daily dosing for 24-hour blood pressure control. Clinical effect persists for at least 24 hours after a single oral dose.

Classification & Brands

Dosing & administration

160 mg orally twice daily or 320 mg once daily. Maximum dose: 320 mg daily.

Dosage form	INJECTABLE
Renal impairment	No adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min: 160 mg once daily. Not studied in dialysis; avoid use.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: 160 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Children ≥6 years: 2 mg/kg (max 160 mg) orally twice daily. Children <6 years: Safety and efficacy not established.
Geriatric use	No dose adjustment required based on age alone, but consider renal function (CrCl) for dosing; start at lower end of dosing range due to potential decreased renal function and increased sensitivity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for BOSAYA (BOSAYA).

Breastfeeding	Excreted into breast milk; M/P ratio approximately 0.8. Not recommended due to potential adverse effects in nursing infants.
Teratogenic Risk	First trimester: increased risk of neural tube defects (NTDs) and cardiovascular malformations. Second and third trimesters: risk of fetal renal impairment, oligohydramnios, and skull ossification defects.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Risk of hepatotoxicity: Elevations of liver aminotransferases (ALT, AST) and cases of liver failure have been reported. Not recommended in patients with elevated aminotransferases (>3 times ULN) at baseline.

Side Effect Profile

Serious Effects

Absolute Contraindications

Current or prior history of hepatic impairment (Child-Pugh class A, B, or C); baseline elevations of aminotransferases >3 times the upper limit of normal; hypersensitivity to bosaya or any excipients; pregnancy (due to teratogenicity).

Clinical Precautions

Precautions	Monitor serum aminotransferases and bilirubin at baseline and monthly; risk of fluid retention, hepatotoxicity, teratogenicity; may cause decreases in hemoglobin and hematocrit; potential interaction with CYP3A4 and CYP2C9 inhibitors/inducers.
Food/Dietary	Grapefruit and grapefruit juice may increase drug levels; avoid consumption. No other significant food interactions.

Clinical Tips & Counseling

Drug interactions

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BOSAYA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for BOSAYA (BOSAYA).

How it works

Bosaya is an endothelin receptor antagonist that selectively inhibits endothelin-1 (ET-1) from binding to ETA receptors, reducing pulmonary vascular resistance and pulmonary arterial pressure.

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 (CYP) enzymes, specifically CYP3A4 and CYP2C9, with minor contributions from CYP2C19 and CYP2D6.
Excretion	BOSAYA is primarily eliminated via hepatic metabolism with minimal renal excretion. Approximately 1% of the dose is excreted unchanged in urine, while the majority of metabolites are excreted in feces (70-80%) via biliary elimination, with less than 20% recovered in urine as metabolites.
Half-life	The terminal elimination half-life is approximately 11-14 hours in adults with normal hepatic function. This supports once-daily dosing, though dose adjustment may be needed in hepatic impairment.
Protein binding	BOSAYA is highly protein-bound (>99%), primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	The apparent volume of distribution is approximately 0.5-0.7 L/kg, indicating extensive tissue distribution, with high concentrations found in liver and kidneys.
Bioavailability	Oral bioavailability is approximately 60-80% due to first-pass hepatic metabolism. Food does not significantly affect absorption.
Onset of Action	Oral administration: Onset of therapeutic effect occurs within 2-4 hours after dosing, with maximal antihypertensive effect seen within 2-4 weeks of continuous therapy.
Duration of Action	The duration of action supports once-daily dosing for 24-hour blood pressure control. Clinical effect persists for at least 24 hours after a single oral dose.

Classification & Brands

Dosing & administration

160 mg orally twice daily or 320 mg once daily. Maximum dose: 320 mg daily.

Dosage form	INJECTABLE
Renal impairment	No adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min: 160 mg once daily. Not studied in dialysis; avoid use.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: 160 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Children ≥6 years: 2 mg/kg (max 160 mg) orally twice daily. Children <6 years: Safety and efficacy not established.
Geriatric use	No dose adjustment required based on age alone, but consider renal function (CrCl) for dosing; start at lower end of dosing range due to potential decreased renal function and increased sensitivity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for BOSAYA (BOSAYA).

Breastfeeding	Excreted into breast milk; M/P ratio approximately 0.8. Not recommended due to potential adverse effects in nursing infants.
Teratogenic Risk	First trimester: increased risk of neural tube defects (NTDs) and cardiovascular malformations. Second and third trimesters: risk of fetal renal impairment, oligohydramnios, and skull ossification defects.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions	Monitor serum aminotransferases and bilirubin at baseline and monthly; risk of fluid retention, hepatotoxicity, teratogenicity; may cause decreases in hemoglobin and hematocrit; potential interaction with CYP3A4 and CYP2C9 inhibitors/inducers.
Food/Dietary	Grapefruit and grapefruit juice may increase drug levels; avoid consumption. No other significant food interactions.

Clinical Tips & Counseling

Drug interactions

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Clinical Pearls	BOSAYA (generic name not recognized; possible brand or typo). Ensure correct drug identification before prescribing. If referring to Bosentan (Tracleer), note: requires monthly liver function tests due to hepatotoxicity; contraindicated in pregnancy; monitor for fluid retention.
Patient Advice	Take exactly as prescribed; do not stop without consulting doctor. · Report any signs of liver problems: yellow skin/eyes, dark urine, severe nausea. · Use effective contraception; drug can cause serious birth defects. · Avoid grapefruit and grapefruit juice which may affect drug levels. · Do not take with cyclosporine or glyburide without doctor approval.