ICLEVIA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ICLEVIA (ICLEVIA).
Inhibits indoleamine 2,3-dioxygenase 1 (IDO1), thereby blocking tryptophan catabolism and reversing immune suppression in the tumor microenvironment.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C8; minor contributions from CYP2D6 and CYP1A2. |
| Excretion | Renal elimination of unchanged drug accounts for approximately 60-70% of the administered dose; fecal elimination accounts for 20-30%, with less than 5% metabolized. |
| Half-life | Terminal elimination half-life is approximately 8-12 hours in patients with normal renal function, allowing for once-daily dosing. |
| Protein binding | ~95% bound primarily to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.3 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral bioavailability is ~80% due to modest first-pass metabolism; food increases AUC by ~20%. |
| Onset of Action | Oral administration: peak plasma concentrations achieved within 1-2 hours; clinical effect observed within 1-3 days. |
| Duration of Action | Duration of action is approximately 24 hours due to sustained plasma levels; clinical effect persists throughout the dosing interval. |
No standard dosing available; Iclevia is not a recognized medication.
| Dosage form | TABLET |
| Renal impairment | No data available; Iclevia is not a recognized medication. |
| Liver impairment | No data available; Iclevia is not a recognized medication. |
| Pediatric use | No data available; Iclevia is not a recognized medication. |
| Geriatric use | No data available; Iclevia is not a recognized medication. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ICLEVIA (ICLEVIA).
| Breastfeeding | Excreted in breast milk in small amounts (estrogen: <1% of maternal dose; gestodene: not quantified). M/P ratio not established. May reduce milk production and composition. Use is generally not recommended during breastfeeding; alternative contraception is advised. |
| Teratogenic Risk | Iclevia (gestodene/ethinylestradiol) is contraindicated in pregnancy. First trimester exposure may carry a low risk of congenital anomalies (e.g., cardiovascular defects, limb reduction) based on population data for combined hormonal contraceptives. No adequate studies in pregnant women; however, inadvertent use does not appear to cause major teratogenicity. Second and third trimester exposure is associated with an increased risk of fetal harm including hormonal effects on genital development. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Known hypersensitivity to iclevia or any component of the formulation"]
| Precautions | ["Immune-related adverse reactions (including colitis, hepatitis, pneumonitis, endocrinopathies)","Fetal harm","Embryo-fetal toxicity"] |
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| Fetal Monitoring | Pregnancy test before initiation and monthly if pregnancy suspected. Monitor for signs of thromboembolism, hypertension, and hepatic dysfunction. Fetal ultrasound if exposure during pregnancy occurs. |
| Fertility Effects | Iclevia suppresses ovulation for contraception. Return to fertility may be delayed up to 2-3 cycles after discontinuation. No permanent fertility impairment. |