Mulpleta (lusutrombopag)
Thrombopoietic Growth Factors Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Lusutrombopag is a small molecule thrombopoietin receptor agonist (TPO-RA).
Lusutrombopag is a small molecule thrombopoietin receptor agonist (TPO-RA). The drug interacts with the transmembrane domain of the TPO receptor and stimulates proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, resulting in an increased production of platelets.
Lusutrombopag increases platelet counts in an exposure-dependent manner. In patients with chronic liver disease and thrombocytopenia receiving a lusutrombopag dosage of 3 mg daily, the mean maximum platelet count without platelet transfusion was 86,900/mm3 and the median time to reach the maximum platelet count was 12 days (range: 5-35 days).
The pharmacokinetics of lusutrombopag are dose-proportional over a single-dose range of 1-50 mg. Following oral administration in patients with chronic liver disease, peak plasma lusutrombopag concentrations occur at 6-8 hours. Following multiple-dose administration, steady state concentrations are reached after 5 days with a systemic accumulation ratio of approximately 2.
Administration with a high-fat meal has no effect on lusutrombopag pharmacokinetics. Lusutrombopag is highly bound (>99%) to plasma proteins. The drug is metabolized principally by cytochrome P-450 (CYP) isoenzymes, including CYP4A11.
Following administration of a radiolabeled dose of lusutrombopag, 83% of the dose was recovered in feces (14% as unchanged drug) and approximately 1% was present in urine. Hemodialysis is not expected to affect elimination of the drug. The terminal elimination half-life of lusutrombopag is approximately 27 hours in healthy individuals.
USES: This medication is used by people with chronic liver disease and a certain blood disorder (low platelet count) who are scheduled to have a medical or dental procedure. Having a low platelet count increases the risk of too much bleeding during certain procedures. This medication increases the production of platelets by your body to help prevent too much bleeding from the procedure.
Generic name: lusutrombopag
Pronunciation: (LOO-soo-TROM-boe-pag)
Drug class: Thrombopoietic Growth Factors
Therapeutic class: Hematological Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Mulpleta
Indications
The following indications are listed for Mulpleta:
- Thrombocytopenia Associated With Chronic Hepatitis
Dosing
In patients with chronic liver disease and thrombocytopenia scheduled to undergo a procedure, the recommended dosage of lusutrombopag is 3 mg once daily for 7 days.
If a dose is missed, it should be administered as soon as it is remembered on the same day. The next dose should be administered at the regularly scheduled time the following day.
Lusutrombopag should not be used to normalize platelet counts.
Lusutrombopag is administered orally once daily for 7 days without regard to food.
The drug should be initiated 8-14 days prior to the scheduled procedure; patients should undergo their procedure 2-8 days after the last dose of the drug.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Mulpleta 3 Mg Tablet | Maintenance | Take 1 tablet (3 mg) by oral route once daily for 7 days beginning 8-14 days prior to procedure. |
No dosing information is available for this tab.
Drug interactions
Lusutrombopag is metabolized by cytochrome P-450 (CYP) isoenzymes, including CYP4A11. In vitro studies indicate that lusutrombopag has low potential to inhibit CYP isoenzymes (1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4/5). Lusutrombopag does not induce CYP1A2, CYP2C9, or CYP3A4, or uridine diphosphate-glucuronosyltransferase (UGT) enzymes UGT1A3, UGT1A6, or UGT2B7 in vitro.
In vitro studies indicate that lusutrombopag is a substrate of p-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). The drug also has a low potential to inhibit P-gp, BCRP, organic anion transporting polypeptide (OATP) 1B or 1B3, organic cation transporter (OCT) 1 or 2, organic anion transporter (OAT) 1 or 3, multidrug and toxin extrusion transporter (MATE) 1 or 2K, or bile salt export pump (BSEP).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
- Lactation
- Thromboembolic disorder
- Antithrombin III deficiency
- Factor V leiden mutation
- Protein C deficiency disease
- Prothrombin g20210A mutation
Adverse reactions
The most common adverse effect reported in >=3% of patients with chronic liver disease receiving lusutrombopag prior to a scheduled procedure in clinical studies was headache.
Rare or Very Rare
- Portal vein thrombosis
- Thromboembolic disorder
- Thrombotic disorder
More Frequent
- Headache disorder
Precautions
No enhanced messaging available.
Safety and efficacy of lusutrombopag have not been established in pediatric patients.
There are no available data to inform a drug-associated risk when lusutrombopag is used during pregnancy. Adverse developmental and postnatal outcomes (e.g., low body weight, teratogenicity, prolonged gestation, delayed growth) were observed in rats administered lusutrombopag orally during organogenesis and the lactation period at dosages resulting in systemic exposures substantially higher (approximately 89 times) than the exposure from the recommended human dosage. Advise pregnant women of the potential fetal risk.
It is not known whether lusutrombopag is distributed into human milk; the drug is distributed into milk in rats. Because of the potential for serious adverse reactions to lusutrombopag in breast-fed infants, advise women not to breast-feed while receiving the drug and for at least 28 days after the last dose. If lusutrombopag is used in a lactating woman, the manufacturer states that breast-feeding should be interrupted and the affected milk discarded during treatment and for 28 days after the last dose.
The effects of the drug on breast-fed infants or on milk production are not known.
Clinical studies of lusutrombopag did not include sufficient numbers of patients >=65 years of age to determine whether geriatric patients respond differently than younger adults. No clinically important differences in responses have been observed between geriatric patients and younger adults in other reported clinical experience.
ICD codes
| Code | Type | Description |
|---|---|---|
| Thrombocytopenia associated with chronic hepatitis | ||
| D69.59 | ICD10CM | Other secondary thrombocytopenia |
| D69.6 | ICD10CM | Thrombocytopenia, unspecified |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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