Dosing & Uses
Dosage Forms & Strengths
tablet
- 70mg
Activated Phosphoinositide 3-kinase Delta Syndrome
Indicated for treatment of immune dysregulation in activated phosphoinositide 3-kinase delta syndrome (APDS), formerly known as PASLI (p110 delta-activating mutation causing senescent T cells, lymphadenopathy, and immunodeficiency) disease, in adults and pediatric patients aged ≥12 years
<45 kg: No recommended dose
≥45 kg: 70 mg PO q12hr
Dosage Modifications
Hepatic impairment
- Extensively (60%) metabolized by the liver; effect of hepatic impairment on pharmacokinetics of leniolisib has not been studied
- Moderate-to-severe: Not recommended
Dosing Considerations
Verify pregnancy status in females of reproductive potential before initiating
Dosage Forms & Strengths
tablet
- 70mg
Activated Phosphoinositide 3-kinase Delta Syndrome
Indicated for treatment of immune dysregulation in activated phosphoinositide 3-kinase delta syndrome (APDS), formerly known as PASLI (p110 delta-activating mutation causing senescent T cells, lymphadenopathy, and immunodeficiency) disease, in adults and pediatric patients aged ≥12 years
<12 years: Safety and efficacy not established
≥12 years and ≥45 kg: 70 mg PO q12hr
<45 kg: No recommended dose
Dosage Modifications
Hepatic impairment
- Extensively (60%) metabolized by the liver; effect of hepatic impairment on pharmacokinetics of leniolisib has not been studied
- Moderate-to-severe: Not recommended
Dosing Considerations
Verify pregnancy status in females of reproductive potential before initiating
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- fezolinetant
leniolisib will increase the level or effect of fezolinetant by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Fezolinetant AUC and peak plasma concentration are increased if coadministered with drugs that are weak, moderate, or strong CYP1A2 inhibitors
Serious - Use Alternative (151)
- alosetron
leniolisib will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- alpelisib
leniolisib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- ambrisentan
leniolisib will increase the level or effect of ambrisentan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- amobarbital
amobarbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- armodafinil
armodafinil will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- atogepant
leniolisib will increase the level or effect of atogepant by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- atorvastatin
leniolisib will increase the level or effect of atorvastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- belzutifan
belzutifan will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bendamustine
leniolisib will increase the level or effect of bendamustine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- bexarotene
bexarotene will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bosentan
bosentan will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
leniolisib will increase the level or effect of bosentan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates - butabarbital
butabarbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- caspofungin
leniolisib will increase the level or effect of caspofungin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- cenobamate
cenobamate will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chloramphenicol
chloramphenicol will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chlorothiazide
leniolisib will increase the level or effect of chlorothiazide by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- cimetidine
leniolisib will increase the level or effect of cimetidine by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- clarithromycin
clarithromycin will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- clomipramine
leniolisib will increase the level or effect of clomipramine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- clozapine
leniolisib will increase the level or effect of clozapine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- cobicistat
cobicistat will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- conivaptan
conivaptan will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dabrafenib
dabrafenib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- darunavir
darunavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- daunorubicin
leniolisib will increase the level or effect of daunorubicin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- digoxin
leniolisib will increase the level or effect of digoxin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- dipyridamole
leniolisib will increase the level or effect of dipyridamole by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- doxorubicin
leniolisib will increase the level or effect of doxorubicin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- duloxetine
leniolisib will increase the level or effect of duloxetine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- duvelisib
duvelisib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- efavirenz
efavirenz will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- elagolix
elagolix will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
leniolisib will increase the level or effect of elagolix by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates - elbasvir/grazoprevir
leniolisib will increase the level or effect of elbasvir/grazoprevir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- eluxadoline
leniolisib will increase the level or effect of eluxadoline by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- enalapril
leniolisib will increase the level or effect of enalapril by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- encorafenib
encorafenib, leniolisib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Encorafenib, an inhibitor and inducer of CYP3A4, may either increase or decrease leniolisib systemic exposure .
- enzalutamide
enzalutamide will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin base
leniolisib will increase the level or effect of erythromycin base by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- erythromycin ethylsuccinate
leniolisib will increase the level or effect of erythromycin ethylsuccinate by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- erythromycin lactobionate
leniolisib will increase the level or effect of erythromycin lactobionate by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- erythromycin stearate
leniolisib will increase the level or effect of erythromycin stearate by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ethinylestradiol
leniolisib will increase the level or effect of ethinylestradiol by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- etrasimod
etrasimod, leniolisib. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Risk of additive immune system effects with etrasimod has not been studied in combination with antineoplastic, immune-modulating, or noncorticosteroid immunosuppressive therapies. Avoid coadministration during and in the weeks following administration of etrasimod.
- etravirine
etravirine will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ezetimibe
leniolisib will increase the level or effect of ezetimibe by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- fexofenadine
leniolisib will increase the level or effect of fexofenadine by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- fluvastatin
leniolisib will increase the level or effect of fluvastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- fluvoxamine
leniolisib will increase the level or effect of fluvoxamine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- fosphenytoin
fosphenytoin will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- glecaprevir/pibrentasvir
leniolisib will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- glyburide
leniolisib will increase the level or effect of glyburide by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- grapefruit
grapefruit will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- imatinib
leniolisib will increase the level or effect of imatinib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- indinavir
indinavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- irinotecan
leniolisib will increase the level or effect of irinotecan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- itraconazole
itraconazole will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivosidenib
ivosidenib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ketoconazole
ketoconazole will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lapatinib
leniolisib will increase the level or effect of lapatinib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- ledipasvir/sofosbuvir
leniolisib will increase the level or effect of ledipasvir/sofosbuvir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- leflunomide
leniolisib will increase the level or effect of leflunomide by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- lenvatinib
leniolisib will increase the level or effect of lenvatinib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- letermovir
leniolisib will increase the level or effect of letermovir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- levoketoconazole
levoketoconazole will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lonafarnib
lonafarnib will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lopinavir
lopinavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lorlatinib
lorlatinib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lovastatin
leniolisib will increase the level or effect of lovastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mavacamten
mavacamten will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- methotrexate
leniolisib will increase the level or effect of methotrexate by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- mexiletine
leniolisib will increase the level or effect of mexiletine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- mifepristone
mifepristone will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitapivat
mitapivat will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitoxantrone
leniolisib will increase the level or effect of mitoxantrone by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- mobocertinib
mobocertinib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- modafinil
modafinil will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nafcillin
nafcillin will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nefazodone
nefazodone will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nelfinavir
nelfinavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nitrofurantoin
leniolisib will increase the level or effect of nitrofurantoin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- olanzapine
leniolisib will increase the level or effect of olanzapine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- olmesartan
leniolisib will increase the level or effect of olmesartan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- olutasidenib
olutasidenib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- osimertinib
leniolisib will increase the level or effect of osimertinib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- ozanimod
leniolisib will increase the level or effect of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- paclitaxel
leniolisib will increase the level or effect of paclitaxel by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- pantoprazole
leniolisib will increase the level or effect of pantoprazole by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- pazopanib
leniolisib will increase the level or effect of pazopanib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- penicillin G benzathine
leniolisib will increase the level or effect of penicillin G benzathine by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- pentobarbital
pentobarbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pexidartinib
pexidartinib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenobarbital
phenobarbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pirfenidone
leniolisib will increase the level or effect of pirfenidone by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration, decrease pirfenidone dose
- pitavastatin
leniolisib will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- pomalidomide
leniolisib will increase the level or effect of pomalidomide by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration, decrease pomalidomide dose
- posaconazole
posaconazole will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pravastatin
leniolisib will increase the level or effect of pravastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- primidone
primidone will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ramelteon
leniolisib will increase the level or effect of ramelteon by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- rasagiline
leniolisib will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration, decrease rasagiline dose
- repaglinide
leniolisib will increase the level or effect of repaglinide by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- revefenacin
leniolisib will increase the level or effect of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- rifabutin
rifabutin will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifapentine
rifapentine will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- riluzole
leniolisib will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- rimegepant
leniolisib will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- riociguat
leniolisib will increase the level or effect of riociguat by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- ritonavir
ritonavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ropinirole
leniolisib will increase the level or effect of ropinirole by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. If unable to avoid coadministration, decrease ropinirole dose
- rosuvastatin
leniolisib will increase the level or effect of rosuvastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- rucaparib
rucaparib will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- saquinavir
saquinavir will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- secobarbital
secobarbital will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- selexipag
leniolisib will increase the level or effect of selexipag by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- selumetinib
leniolisib will increase the level or effect of selumetinib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- simvastatin
leniolisib will increase the level or effect of simvastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- sofosbuvir
leniolisib will increase the level or effect of sofosbuvir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- sotorasib
sotorasib will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- St John's Wort
St John's Wort will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- stiripentol
stiripentol, leniolisib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Stiripentol, an inhibitor and inducer of CYP3A4, may either increase or decrease leniolisib systemic exposure .
- sulbactam/durlobactam
leniolisib will increase the level or effect of sulbactam/durlobactam by Other (see comment). Avoid or Use Alternate Drug. Sulbactam is predicted to have active secretion by OATP1 as a significant portion of total clearance; therefore, inhibition of OAT1 may increase sulbactam plasma concentrations
- sulfasalazine
leniolisib will increase the level or effect of sulfasalazine by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- talazoparib
leniolisib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- tasimelteon
leniolisib will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- telmisartan
leniolisib will increase the level or effect of telmisartan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- telotristat ethyl
telotristat ethyl will decrease the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tenofovir AF
leniolisib will increase the level or effect of tenofovir AF by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- tenofovir DF
leniolisib will increase the level or effect of tenofovir DF by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- theophylline
leniolisib will increase the level or effect of theophylline by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- tizanidine
leniolisib will increase the level or effect of tizanidine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid leniolisib with CYP1A2 substrates that have a narrow therapeutic index
- topotecan
leniolisib will increase the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- troglitazone
leniolisib will increase the level or effect of troglitazone by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- tucatinib
tucatinib will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ubrogepant
leniolisib will increase the level or effect of ubrogepant by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- valsartan
leniolisib will increase the level or effect of valsartan by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- velpatasvir
leniolisib will increase the level or effect of velpatasvir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- vemurafenib
leniolisib will increase the level or effect of vemurafenib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- voriconazole
voriconazole will increase the level or effect of leniolisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- voxilaprevir
leniolisib will increase the level or effect of voxilaprevir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these substrates
Monitor Closely (22)
- adenovirus types 4 and 7 live, oral
leniolisib decreases effects of adenovirus types 4 and 7 live, oral by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- BCG vaccine live
leniolisib decreases effects of BCG vaccine live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- cholera vaccine
leniolisib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- dengue vaccine
leniolisib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- Ebola Zaire vaccine
leniolisib decreases effects of Ebola Zaire vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- influenza virus vaccine quadrivalent, intranasal
leniolisib decreases effects of influenza virus vaccine quadrivalent, intranasal by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- measles (rubeola) vaccine
leniolisib decreases effects of measles (rubeola) vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- measles mumps and rubella vaccine, live
leniolisib decreases effects of measles mumps and rubella vaccine, live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- measles, mumps, rubella and varicella vaccine, live
leniolisib decreases effects of measles, mumps, rubella and varicella vaccine, live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- melatonin
leniolisib will increase the level or effect of melatonin by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Monitor melatonin effects if coadministered with moderate CYP1A2 inhibitors
- momelotinib
leniolisib increases toxicity of momelotinib by Other (see comment). Use Caution/Monitor. Comment: OATP1B1/B3 inhibitor increases momelotinib (OATP1B1/B3 subtrate) plasma concentrations, which may increase the risk of adverse reactions with momelotinib.
- poliovirus vaccine live oral trivalent
leniolisib decreases effects of poliovirus vaccine live oral trivalent by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- rotavirus oral vaccine, live
leniolisib decreases effects of rotavirus oral vaccine, live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- rubella vaccine
leniolisib decreases effects of rubella vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- smallpox (vaccinia) and monkeypox vaccine, live, nonreplicating
leniolisib decreases effects of smallpox (vaccinia) vaccine, attenuated by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- smallpox (vaccinia) vaccine, attenuated
leniolisib decreases effects of smallpox (vaccinia) vaccine, attenuated by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- smallpox (vaccinia) vaccine, live
leniolisib decreases effects of smallpox (vaccinia) vaccine, live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- typhoid polysaccharide vaccine
leniolisib decreases effects of typhoid polysaccharide vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- typhoid vaccine live
leniolisib decreases effects of typhoid vaccine live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- varicella virus vaccine live
leniolisib decreases effects of varicella virus vaccine live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- yellow fever vaccine
leniolisib decreases effects of yellow fever vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
- zoster vaccine live
leniolisib decreases effects of zoster vaccine live by immunosuppressive effects; risk of infection. Use Caution/Monitor. Live, attenuated vaccinations may be less effective if administered during leniolisib treatment.
Minor (0)
Adverse Effects
>10%
ANC 500-1500 cells/microL (33%)
Headache (24%)
Sinusitis (19%)
Atopic dermatitis (14%)
1-10%
Tachycardia (10%)
Diarrhea (10%)
Fatigue (10%)
Pyrexia (10%)
Back pain (10%)
Neck pain (10%)
Alopecia (10%)
Warnings
Contraindications
None
Cautions
Based on findings in animals, may cause fetal harm when administered to pregnant females
Drug interaction overview
- Substrate of CYP3A4
- Inhibitor of CYP1A2, BCRP, OATP1B1, OATP1B3
-
Vaccines
- Caution, monitor
- Live, attenuated vaccinations may be less effective if administered during leniolisib treatment
-
Strong CYP3A4 inhibitors
- Avoid coadministration
- Leniolisib exposure was increased 2-fold when coadministered with itraconazole, a strong CYP3A4 inhibitor
-
Strong and moderate CYP3A4 inducers
- Avoid coadministration
- Strong and moderate CYP3A4 inducers may reduce leniolisib systemic exposure and thus reduced leniolisib efficacy
-
Sensitive CYP1A2 substrates
- Avoid coadministration
- Coadministration may increase CYP1A2 systemic exposure
- Avoid with CYP1A2 substrates that have a narrow therapeutic index
-
BCRP, OATP1B1, and OAP1B3 substrates
- Avoid coadministration
- Effect of leniolisib on BCRP, OATP1B1, and OATP1B3 substrates has not been studied clinically
- Owing to possible increase in systemic exposure of these substrates, avoid concomitant use
Pharmacology
Mechanism of Action
Inhibits phosphoinositide 3-kinase (PI3K) delta by blocking the active binding site of PI3K-delta; this inhibits the signaling pathways that lead to increased production of PIP3, hyperactivity of the downstream mTOR/AKT pathway, and to the dysregulation of B and T cells
Absorption
Peak plasma time: 1 hr
Steady-state reached: ~2-3 days
Distribution
Protein bound: 94.5%
Vd: 28.5 L
Metabolism
60% metabolized by liver, with CYP3A4 being the most predominant enzyme involved (94.5%) with minor contribution of CYP3A5, CYP1A2, and CYP2D6
Elimination
Terminal half-life: ~10 hr
Excretion: Feces 67%; urine 25.5% (6.32% unchanged leniolisib)
Administration
Oral Administration
May take with or without food
Missed or vomited dose
- Dose missed by >6 hr: Wait and take next dose at the usual time
-
Vomited dose
- ≤1 hr after administration: Take as soon as possible
- >1 hr after administration: Wait and take the next dose at the usual time
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Do not refrigerate
Store and dispense in original container
Images
Formulary
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