Dosing & Uses
Dosage Forms & Strengths
subcutaneous implant
- 16mg/implant
Phototoxicity/Anaphylaxis & Erythropoietic Protoporphyria
Indicated for prevention of phototoxicity and anaphylactoid reactions in adults with erythropoietic protoporphyria (EPP)
16 mg implanted SC q2Months
Safety and efficacy not established
Adverse Effects
>10%
Implant site reaction (21%)
Nausea (19%)
1-10%
Oropharyngeal pain (7%)
Fatigue (6%)
Skin hyperpigmentation (4%)
Dizziness (4%)
Melanocytic nevus (4%)
Respiratory tract infection (4%)
Somnolence (2%)
Nonacute porphyria (2%)
Skin irritation (2%)
Warnings
Contraindications
None
Cautions
Owing to its pharmacologic effect, afamelanotide may lead to generalized increased skin pigmentation and darkening of preexisting nevi and ephelides; twice-yearly full-body skin examination recommended to monitor preexisting and new skin pigmentary lesions
Pregnancy & Lactation
Pregnancy
No data are available regarding use in pregnant women to evaluate for any drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcome
Animal data
In animal reproductive and development toxicity studies, no adverse developmental effects were observed with administration during organogenesis to pregnant rats at SC doses up to 12 times the maximum recommended human dose (MRHD)
Lactation
No data are available on the presence of afamelanotide or any of its metabolites in human or animal milk, effects on the breastfed infant, or on milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Erythropoietic protoporphyria is a rare disorder caused by mutations leading to impaired activity of ferrochelatase, an enzyme involved in heme production; decreased ferrochelatase activity leads to protoporphyrin IX (PPIX) accumulation in the body; light reaching the skin can react with PPIX, causing intense skin pain and skin changes (eg, redness, thickening)
Afamelanotide, a melanocortin-1 receptor (MC1-R) agonist, increases production of eumelanin (the most common type of melanin) in the skin independent of exposure to sunlight or artificial light sources
Absorption
Peak plasma time: 36 hr
Peak plasma concentration: 3.7 ng/mL
AUC: 42.6 hr⋅ng/mL
Metabolism
Not fully characterized; may undergo hydrolysis
Elimination
Half-life: 15 hr
Administration
SC Implant Preparation
Equipment required
- Afamelanotide implant
- SFM implantation cannula (contact manufacturer for other suitable implantation devices)
- Sterile gloves
- Local anesthetic, needle, and syringe
- Blunt forceps suitable for removing implant from vial
- Sterile gauze, adhesive bandage, pressure bandage
SC Implant Administration
Also see prescribing information for instructions and diagrams
Step 1
- Remove implant from refrigerator and allow to gradually warm up to ambient temperature
- Remove the seal and stopper from the glass vial containing implant; remove implant from vial using the blunt forceps under aseptic conditions and place on sterile gauze
Step 2
- Position patient in a comfortable reclined supine position
- Identify the insertion site 3-4 cm above the anterior suprailiac crest and disinfect the skin surface
Step 3 (optional)
- Anesthetize insertion area if deemed necessary and in consultation with the patient
Step 4
- While pinching skin at insertion site, insert the cannula with the bevel facing upwards (away from the abdomen) at a 30-45º angle into the SC layer
- Advance the cannula 2 cm into the SC layer
Step 5
- Remove stylet (obturator) from the cannula, maintaining aseptic precautions
- Load the implant into the cannula
- Using the stylet (obturator), gently push the implant down the full length of the cannula’s shaft
Step 6
- Apply pressure to implant site while removing the stylet (obturator) and cannula
- Verify that no implant or implant portion remains in the cannula
Step 7
- Verify the correct insertion and placement of the implant by palpating the skin overlying the implant
Step 8
- Apply dressing to the insertion site
- Leave dressing in place for 24 hr
Step 9
- Monitor the patient for 30 minutes after implant administration
Storage
Refrigerate at 2-8ºC (36-46ºF)
Protect from light
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.