Xianluoli Sirolimus Gel

1. Indications and Usage
Facial Angiofibromas Associated with Tuberous Sclerosis Complex (TSC):
Indicated for the topical treatment of facial angiofibromas associated with tuberous sclerosis complex in adult and pediatric patients 6 years of age and older .
2. Dosage and Administration
Route of Administration:
For TOPICAL USE ONLY. Not for oral, ophthalmic, or vaginal use.
Recommended Dosage:
Frequency: Apply a thin layer to the affected facial skin twice daily (every 12 hours).
Amount:
Adults and children ≥12 years: Approximately 2.5 cm strip length per application.
Children 6–11 years: Approximately 2.0 cm strip length per application .
Application: Wash and dry the face before application. Do not cover with occlusive dressings .
Storage:
Store under refrigeration at 2°C–8°C (36°F–46°F). Protect from light .
3. Mechanism of Action
mTOR Inhibition:
Tuberous sclerosis complex is caused by mutations in TSC1 or TSC2 genes, leading to hyperactivation of the mammalian target of rapamycin (mTOR).
Pathway Suppression:
Sirolimus binds to FKBP12 to form a complex that inhibits mTOR activation. This suppresses cell proliferation and angiogenesis, thereby reducing the size and number of angiofibromas .
4. Safety and Warnings
Hypersensitivity:
Do not use in patients with a history of hypersensitivity to sirolimus or any excipients. Reactions may include angioedema or exfoliative dermatitis .
Avoid Contact with Eyes and Mucous Membranes:
Accidental contact may cause eye irritation. Wash with water immediately if contact occurs .
Delayed Wound Healing:
Sirolimus inhibits cell proliferation; avoid applying to open wounds or broken skin .
5. Adverse Reactions
Most Common:
Dermatologic: Dry skin (30.4%), application site irritation (27.0%), acne (10.1%), pruritus (8.8%), and acneiform dermatitis .
Ocular: Eye irritation (5.4%) .
Systemic Absorption:
Systemic absorption is low, and significant systemic toxicities associated with oral sirolimus (e.g., severe immunosuppression) are rare .
6. Drug Interactions
Local vs. Systemic:
Due to low systemic absorption, clinically significant drug interactions are unlikely with topical use.
Oral Sirolimus:
No data available on concurrent use with oral sirolimus or other mTOR inhibitors.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Sirolimus.
Strength: 0.2% (10 g: 20 mg).
Appearance: Clear gel.
Storage: Refrigerated .