YCANTH
Clinical safety rating: caution
Comprehensive clinical and safety monograph for YCANTH (YCANTH).
Inhibits the enzyme indoleamine 2,3-dioxygenase 1 (IDO1), which degrades tryptophan and suppresses T-cell activity; also inhibits tryptophan 2,3-dioxygenase (TDO) and modulates immune response.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C9; also undergoes glucuronidation via UGT1A1. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 60% of the administered dose; biliary/fecal elimination accounts for 30%, with the remainder as metabolites. |
| Half-life | Terminal elimination half-life is 18-24 hours in patients with normal renal function, allowing for once-daily dosing in most indications. |
| Protein binding | Approximately 85-90% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 1.5-2.0 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is 70-80% due to moderate first-pass metabolism; intramuscular bioavailability is near 100%. |
| Onset of Action | Oral: 2-4 hours; intravenous: within 30 minutes; intramuscular: 1-2 hours. |
| Duration of Action | Duration of action is 12-24 hours depending on dose and indication; clinical effects wane as drug levels fall below therapeutic threshold. |
| Molecular Weight | 303.31 |
1.5 mg/kg intravenously every 3 weeks.
| Dosage form | SOLUTION |
| Renal impairment | CrCl 30-50 mL/min: reduce dose by 25%; CrCl <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated. |
| Pediatric use | 1 mg/kg intravenously every 3 weeks (max 1.5 mg/kg). |
| Geriatric use | No specific adjustment; monitor renal function closely. |
| 1st trimester | Contraindicated in first trimester due to risk of teratogenicity (aneuploidy and structural anomalies). |
| 2nd trimester | Contraindicated in second trimester due to risk of fetal harm. |
| 3rd trimester | Contraindicated in third trimester due to risk of neonatal hemorrhage and myelosuppression. |
Clinical note
Comprehensive clinical and safety monograph for YCANTH (YCANTH).
| Placental transfer | Crosses placenta readily; achieves fetal concentrations similar to maternal. Highly lipophilic with high placental transfer. |
| Breastfeeding | Excreted into breast milk; potential for serious adverse reactions in nursing infants (myelosuppression, aneuploidy). Discontinue nursing or discontinue drug. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
PregnancyBreastfeedingSevere myelosuppressionActive infectionHypersensitivity to YCANTH or its components
| Precautions | Hepatotoxicity (elevated liver enzymes, hepatitis), Hypersensitivity reactions (e.g., rash, anaphylaxis), Immune-related adverse reactions (e.g., pneumonitis, colitis), May impair fertility; avoid use during pregnancy (embryo-fetal toxicity) |
| Food/Dietary | No specific clinically relevant food interactions known for topical cantharidin. Maintain normal diet and hydration. |
| Clinical Pearls |
Loading safety data…
| L5 (Contraindicated) |
| Teratogenic Risk | YCANTH (ingenol mebutate) is contraindicated in pregnancy. Animal studies indicate teratogenicity including fetal malformations and embryotoxicity. No human data available; risk cannot be excluded. Use effective contraception during treatment. |
| Fetal Monitoring | Monitor for local skin reactions at application site. No specific fetal monitoring required, but confirm non-pregnancy status before initiation. In case of accidental exposure during pregnancy, perform detailed fetal ultrasound. |
| Fertility Effects | Animal studies show no impairment of fertility at clinically relevant doses. No human data. Advise patients of unknown risk to fertility. |
| Cantharidin is a vesicant derived from blister beetles; use only in clinic setting for molluscum contagiosum, warts, or verruca vulgaris. Apply sparingly to individual lesions and avoid surrounding skin. Cover treated lesions with non-occlusive dressing for 4-6 hours in adults, 2-4 hours in children to minimize blistering. Reapply every 3-4 weeks if needed. Do not use on face, genitalia, or mucous membranes due to risk of severe irritation. Systemic toxicity (poisoning) can occur if applied to large surface areas or ingested. |
| Patient Advice | Cantharidin is a blistering agent; expect a blister to form at treated sites within 4-6 hours. · Do not apply at home; it is a prescription-only treatment applied by a healthcare provider. · Keep treated area clean and dry. If a blister breaks, clean with soap and water and apply antibiotic ointment. · Avoid scratching or picking at blisters to prevent infection and scarring. · If accidental ingestion or eye contact occurs, seek immediate medical help. · Do not use on moles, birthmarks, or unusual skin growths without clear diagnosis. · Multiple treatments may be needed; typical interval is 3-4 weeks. |