Your Health, We Care
Another NamePS-433540, RE-021, DARA-a, 斯帕森坦,司帕生坦
IndicationsSparsentan is suitable for reducing proteinuria in adult patients with primary immunoglobulin A nephropathy.
Reg No.10 L 1036/23
Inspection NO.2582-23
The original manufacturer of Sparsentan is Gilead Sciences, and Sparsentan was approved for market by the US Food and Drug Administration (FDA) in April 2022.
This approval marks the recognition of Sparsentan's potential in treating specific diseases and provides patients with new treatment options.
Sparsentan is an oral dual endothelin angiotensin receptor antagonist designed to treat a range of diseases associated with overactivation of both endothelin type A (ETA) and angiotensin II type 1 (AT1) receptors by simultaneously blocking their effects.
Sparsentan
Sparsentan is suitable for reducing proteinuria in adult patients with primary immunoglobulin A nephropathy.
Based on data from animal reproductive toxicity studies, Sparsentan can cause fetal harm, including birth defects and fetal death, when administered to a pregnant patient and is contraindicated during pregnancy. Available data from reports of pregnancy in clinical trials with Sparsentan are insufficient to identify a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of sparsentan to pregnant rats throughout organogenesis at 10-times the maximum recommended human dose (MRHD) in mg/day caused teratogenic effects in rats, including craniofacial malformations, skeletal abnormalities, increased embryo-fetal lethality, and reduced fetal weights. Advise pregnant patients of the potential risk to the fetus.
There are no data on the presence of sparsentan in human milk, the effects on the breastfed infant, or the effect on milk production. Because of the potential for adverse reactions, such as hypotension in breastfed infants, advise patients not to breastfeed during treatment with Sparsentan.
Based on data from animal reproductive toxicity studies, Sparsentan can cause fetal harm, including birth defects and fetal death, when administered to a pregnant patient and is contraindicated during pregnancy.
Patients who can become pregnant who are using Sparsentan must use an effective method of contraception prior to initiation of treatment, during treatment, and for one month after discontinuation of treatment with Sparsentan to prevent pregnancy.
The safety and efficacy of Sparsentan in pediatric patients have not been established.
Of the total number of subjects in the PROTECT study of Sparsentan, 15 (7.4%) were 65 and older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.
Avoid use of Sparsentan in patients with any hepatic impairment (Child-Pugh class A-C) because of the potential risk of serious liver injury.
There is no experience with overdose with Sparsentan. Sparsentan has been given in doses up to 1600 mg/day in healthy volunteers, or up to 400 mg/day in patients. Overdose of Sparsentan may result in decreased blood pressure. In the event of an overdose, standard supportive measures should be taken, as required. Dialysis is unlikely to be effective because sparsentan is highly protein-bound.
Store at 20°C to 25°C (68°F to 77°F), excursions permitted to 15°C to 30°C (59°F to 86°F). Store Sparsentan in its original container.
The pharmacokinetics of sparsentan are presented as geometric mean (% coefficient of variation) unless otherwise specified. The Cmax and AUC of sparsentan increase less than proportionally following administration of single doses of 200 mg to 1600 mg. Sparsentan showed time-dependent pharmacokinetics which may be related to the drug inducing its own metabolism over time. Steady-state plasma levels are reached within 7 days with no accumulation of exposure at the approved recommended dosage. Following a single oral dose of 400 mg sparsentan, the mean Cmax and AUC are 6.97 μg/mL and 83 μg×h/mL, respectively. Following daily doses of 400 mg sparsentan, the steady-state mean Cmax and AUC are 6.47 μg/mL and 63.6 μg×h/mL, respectively.
from FDA，2023.02
