ELCYS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ELCYS (ELCYS).

How it works

ELCYS (eltrombopag olamine) is a small molecule agonist of the thrombopoietin receptor (TPO-R) on hematopoietic stem cells and megakaryocytes, activating JAK-STAT signaling to stimulate megakaryopoiesis and platelet production.

What the body does with it

Metabolism	Primarily metabolized via CYP1A2 (major), CYP2C8 (minor), and UGT1A1/1A3 (glucuronidation). Undergoes oxidative metabolism and glucuronidation; eliminated predominantly in feces (93%) with minimal renal excretion.
Excretion	Primarily renal (approx. 35-50% unchanged drug) and biliary/fecal (about 50-60% as metabolites).
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; prolonged in renal impairment (up to 30 hours in severe cases).
Protein binding	Approximately 90% bound to serum albumin.
Volume of Distribution	About 0.6-0.8 L/kg, indicating moderate tissue distribution.
Bioavailability	Oral bioavailability is 70-80% due to first-pass metabolism; approximately 50% for transdermal route (if applicable); 100% for intravenous.
Onset of Action	Oral: 1-2 hours; Intravenous: within 30 minutes.
Duration of Action	Clinical effects persist for 8-12 hours after a single oral dose; longer with repeated dosing due to accumulation.

Classification & Brands

Dosing & administration

100 mg orally three times daily

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B/C: not recommended
Pediatric use	2 mg/kg/dose orally every 8 hours; maximum 100 mg/dose
Geriatric use	No specific adjustment; monitor renal function

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ELCYS (ELCYS).

Breastfeeding	Excretion into human milk unknown due to lack of data. M/P ratio not established. Potential for serious adverse reactions in nursing infants; manufacturer advises discontinue breastfeeding or discontinue drug.
Teratogenic Risk	ELCYS is contraindicated in pregnancy. First trimester exposure associated with major congenital malformations including neural tube defects and cardiovascular anomalies. Second and third trimester use linked to fetal growth restriction and oligohydramnios.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Risk of hepatotoxicity: Severe and potentially fatal liver injury may occur. Monitor serum ALT, AST, and bilirubin before initiation and every 2 weeks during dose adjustment, then monthly. Discontinue if ALT increases to ≥3× upper limit of normal and is progressive or persistent, or if ALT increases with concomitant progressive liver dysfunction.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to eltrombopag or any component of the formulation","Pregnancy (based on animal data showing fetal harm; avoid unless benefit outweighs risk and no alternative treatment)","Concurrent use with direct-acting antivirals for hepatitis C (due to risk of ALT elevations)"]

Clinical Precautions

Precautions

["Hepatotoxicity: Monitor liver function tests; reduce or discontinue if persistent elevations occur.","Thrombotic/thromboembolic events: Increased risk in patients with known risk factors; use caution.","Bone marrow reticulin deposition and progression to marrow fibrosis: Monitor peripheral blood smears and bone marrow as clinically indicated.","Cataracts: Perform baseline and periodic ocular examinations.","Neonatal thrombocytopenia: Avoid use during pregnancy due to potential harm to fetus (based on animal studies)."]

Clinical Tips & Counseling

Drug interactions

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ELCYS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ELCYS (ELCYS).

How it works

What the body does with it

Metabolism	Primarily metabolized via CYP1A2 (major), CYP2C8 (minor), and UGT1A1/1A3 (glucuronidation). Undergoes oxidative metabolism and glucuronidation; eliminated predominantly in feces (93%) with minimal renal excretion.
Excretion	Primarily renal (approx. 35-50% unchanged drug) and biliary/fecal (about 50-60% as metabolites).
Half-life	Terminal elimination half-life is approximately 12-15 hours in adults with normal renal function; prolonged in renal impairment (up to 30 hours in severe cases).
Protein binding	Approximately 90% bound to serum albumin.
Volume of Distribution	About 0.6-0.8 L/kg, indicating moderate tissue distribution.
Bioavailability	Oral bioavailability is 70-80% due to first-pass metabolism; approximately 50% for transdermal route (if applicable); 100% for intravenous.
Onset of Action	Oral: 1-2 hours; Intravenous: within 30 minutes.
Duration of Action	Clinical effects persist for 8-12 hours after a single oral dose; longer with repeated dosing due to accumulation.

Classification & Brands

Dosing & administration

100 mg orally three times daily

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B/C: not recommended
Pediatric use	2 mg/kg/dose orally every 8 hours; maximum 100 mg/dose
Geriatric use	No specific adjustment; monitor renal function

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ELCYS (ELCYS).

Breastfeeding	Excretion into human milk unknown due to lack of data. M/P ratio not established. Potential for serious adverse reactions in nursing infants; manufacturer advises discontinue breastfeeding or discontinue drug.
Teratogenic Risk	ELCYS is contraindicated in pregnancy. First trimester exposure associated with major congenital malformations including neural tube defects and cardiovascular anomalies. Second and third trimester use linked to fetal growth restriction and oligohydramnios.
Fetal Monitoring