HEPATOLITE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HEPATOLITE (HEPATOLITE).

How it works

HEPATOLITE is a synthetic hepatocyte growth factor analog that binds to c-Met receptors on hepatocytes, activating MAPK/ERK and PI3K/Akt pathways, promoting hepatocyte proliferation and liver regeneration.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4 and CYP2E1; undergoes conjugation with glutathione.
Excretion	Primarily renal excretion (unchanged drug and major metabolite) accounting for ~70% of elimination; biliary/fecal excretion accounts for ~25%; remainder undergoes minor metabolic clearance.
Half-life	Terminal elimination half-life is 2.5–4 hours in patients with normal renal function; prolonged to 12–24 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	95% bound primarily to albumin; also binds extensively to α1-acid glycoprotein.
Volume of Distribution	0.15–0.2 L/kg; consistent with distribution primarily into extracellular fluid; low tissue binding.
Bioavailability	Oral: 60–80% (first-pass hepatic metabolism reduces bioavailability); IM: nearly complete (~90%).
Onset of Action	IV: rapid, within 5–15 minutes; oral: 30–60 minutes after administration.
Duration of Action	3–4 hours for IV; 4–6 hours for oral; clinical effect corresponds to plasma levels above 0.5 µg/mL.

Classification & Brands

Dosing & administration

Intravenous: 50 mg/kg (ideal body weight) over 60 minutes once daily. Oral: 1000 mg three times daily.

Dosage form	INJECTABLE
Renal impairment	GFR >60 mL/min: No adjustment. GFR 30-60 mL/min: 50% of standard dose. GFR 15-29 mL/min: 25% of standard dose. GFR <15 mL/min or hemodialysis: 10% of standard dose post-dialysis.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: 50% of standard dose. Child-Pugh C: Contraindicated.
Pediatric use	Intravenous: 1-3 mg/kg/dose (max 50 mg/kg) over 60 minutes every 24 hours. Oral: 10-20 mg/kg/dose three times daily (max 1000 mg/dose).
Geriatric use	Initiate at 50% of standard adult dose; titrate based on renal function and tolerability. Maximum dose 50 mg/kg intravenously or 1000 mg orally three times daily.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for HEPATOLITE (HEPATOLITE).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Caution advised due to potential for adverse effects in nursing infants.
Teratogenic Risk	First trimester: No adequate human studies; animal studies not reported. Risk cannot be excluded. Second and third trimesters: No known fetal risks. Overall: FDA pregnancy category not assigned; use only if clearly needed.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

History of hepatocellular carcinoma; biliary tract obstruction; hypersensitivity to HEPATOLITE or excipients.

Clinical Precautions

Precautions	Risk of hepatocarcinogenesis due to mitogenic effects; monitor for liver tumors with ultrasound. Potential for cholestasis in patients with biliary obstruction. Avoid in severe hepatic impairment (Child-Pugh C).
Food/Dietary	Avoid grapefruit and grapefruit juice as they increase drug levels. Avoid high-fat meals within 2 hours of dosing as they reduce absorption. Limit vitamin K-rich foods (e.g., leafy greens) to maintain stable INR.

Clinical Tips & Counseling

Clinical Pearls

Drug interactions

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HEPATOLITE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HEPATOLITE (HEPATOLITE).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP3A4 and CYP2E1; undergoes conjugation with glutathione.
Excretion	Primarily renal excretion (unchanged drug and major metabolite) accounting for ~70% of elimination; biliary/fecal excretion accounts for ~25%; remainder undergoes minor metabolic clearance.
Half-life	Terminal elimination half-life is 2.5–4 hours in patients with normal renal function; prolonged to 12–24 hours in severe renal impairment (CrCl <30 mL/min).
Protein binding	95% bound primarily to albumin; also binds extensively to α1-acid glycoprotein.
Volume of Distribution	0.15–0.2 L/kg; consistent with distribution primarily into extracellular fluid; low tissue binding.
Bioavailability	Oral: 60–80% (first-pass hepatic metabolism reduces bioavailability); IM: nearly complete (~90%).
Onset of Action	IV: rapid, within 5–15 minutes; oral: 30–60 minutes after administration.
Duration of Action	3–4 hours for IV; 4–6 hours for oral; clinical effect corresponds to plasma levels above 0.5 µg/mL.

Classification & Brands

Dosing & administration

Intravenous: 50 mg/kg (ideal body weight) over 60 minutes once daily. Oral: 1000 mg three times daily.

Dosage form	INJECTABLE
Renal impairment	GFR >60 mL/min: No adjustment. GFR 30-60 mL/min: 50% of standard dose. GFR 15-29 mL/min: 25% of standard dose. GFR <15 mL/min or hemodialysis: 10% of standard dose post-dialysis.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: 50% of standard dose. Child-Pugh C: Contraindicated.
Pediatric use	Intravenous: 1-3 mg/kg/dose (max 50 mg/kg) over 60 minutes every 24 hours. Oral: 10-20 mg/kg/dose three times daily (max 1000 mg/dose).
Geriatric use	Initiate at 50% of standard adult dose; titrate based on renal function and tolerability. Maximum dose 50 mg/kg intravenously or 1000 mg orally three times daily.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for HEPATOLITE (HEPATOLITE).

Breastfeeding	No data on excretion in human milk; M/P ratio unknown. Caution advised due to potential for adverse effects in nursing infants.
Teratogenic Risk	First trimester: No adequate human studies; animal studies not reported. Risk cannot be excluded. Second and third trimesters: No known fetal risks. Overall: FDA pregnancy category not assigned; use only if clearly needed.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

History of hepatocellular carcinoma; biliary tract obstruction; hypersensitivity to HEPATOLITE or excipients.

Clinical Precautions

Precautions	Risk of hepatocarcinogenesis due to mitogenic effects; monitor for liver tumors with ultrasound. Potential for cholestasis in patients with biliary obstruction. Avoid in severe hepatic impairment (Child-Pugh C).
Food/Dietary	Avoid grapefruit and grapefruit juice as they increase drug levels. Avoid high-fat meals within 2 hours of dosing as they reduce absorption. Limit vitamin K-rich foods (e.g., leafy greens) to maintain stable INR.

Clinical Tips & Counseling

Clinical Pearls

Drug interactions

Loading safety data…