Acts as an inhibitor of phosphatidylinositol 3-kinase-delta, thereby inhibiting the signaling pathways that lead to increased production of PIP3, hyperactivity of the downstream mTOR/AKT pathway, and dysregulation of B and T cells.
Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme, and minor contribution by the CYP3A5, CYP1A2, and CYP2D6 isoenzymes. Primarily excreted in the feces (67%), with 25.5% excreted in the urine.
Half-Life: 10 hr.
Time/Action Profile⬆⬇
(plasma concentrations)
ROUTE
ONSET
PEAK
DURATION
PO
rapid
1 hr
12 hr
Contraind./Precautions⬆⬇
Contraindicated in:
Moderate or severe hepatic impairment;
OB: Pregnancy;
Lactation: Lactation.
Use Cautiously in:
Rep: Women of reproductive potential;
Pedi: Children <12 yr (safety and effectiveness not established).
PO (Adults and Children ≥12 yr and ≥45 kg): 70 mg twice daily.
Availability⬆⬇
Tablets: 70 mg
Assessment⬆⬇
Monitor for tachycardia, headache, sinusitis, and atopic dermatitis periodically throughout therapy.
Lab Test Considerations:
Verify negative pregnancy test before starting therapy.
Monitor liver enzymes at baseline.
Monitor CBC with differential during therapy May cause mild neutropenia.
Implementation⬆⬇
PO: Administer without regard to food.
Patient/Family Teaching⬆⬇
Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient that if a dose is missed by >6 hr or is vomited >1 hr after dose, wait and take at the next scheduled time. If patient vomits ≤1 hr after dose, retake as soon as possible.
Inform patient that live-attenuated vaccines may be less effective when given during therapy with leniolisib.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Advise women of reproductive potential to use highly effective method of contraception and not to breastfeed during therapy and for 1 week after the last dose. Advise patient to notify health care professional if pregnancy planned or suspected or if breastfeeding.
