afamelanotide

Action and Spectrum

afamelanotide is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH). It is used to treat a condition called erythropoietic protoporphyria (EPP), a rare genetic disorder resulting in the accumulation of protoporphyrin in the skin. When the skin is exposed to sunlight, the protoporphyrin absorbs UV light and causes severe pain, swelling, and skin lesions. 

afamelanotide works by activating the melanocortin one receptor (MC1R), which stimulates the production of melanin in the skin. Melanin is a pigment that absorbs UV light and protects the skin from the harmful effects of sunlight. afamelanotide is thought to work by increasing the production of melanin in the skin, which helps to protect against UV-induced damage. 

The spectrum of afamelanotide includes its effects on skin pigmentation and protection against UV-induced damage. It is used specifically to treat EPP, a rare genetic disorder characterized by sensitivity to sunlight and the accumulation of protoporphyrin in the skin. It is not indicated for use in other conditions 

Drug Interaction

Adverse Reaction

Frequency defined:  

>10% 

Nausea 

Reaction at the implant site 

1-10% 

Fatigue 

Dizziness 

Respiratory tract infections 

Nonacute porphyria 

Oropharyngeal pain 

Skin hyperpigmentation 

Melanocytic nevus 

Somnolence 

Skin irritation 

Black Box Warning

Contraindication / Caution

afamelanotide is contraindicated in people who have had a previous allergic reaction to afamelanotide or any of its components. It should also be used with caution in people with a history of melanoma or other skin cancers, as the drug may increase the risk of developing these conditions. 

It is important to note that afamelanotide is only available through a restricted distribution program and is only indicated for treating adult erythropoietic protoporphyria (EPP). It should only be used under the supervision of a healthcare provider experienced in the management of EPP. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology

afamelanotide is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), a naturally occurring hormone that plays a role in skin pigmentation. afamelanotide activates the melanocortin one receptor (MC1R), which stimulates the production of melanin in the skin. Melanin is a pigment that absorbs UV light and protects the skin from the harmful effects of sunlight. 

Pharmacodynamics 

afamelanotide is a synthetic hormone designed to mimic the effects of alpha-melanocyte-stimulating hormone (alpha-MSH). Alpha-MSH is a hormone the pituitary gland produces that regulates melanin production in the skin. 

afamelanotide works by activating the skin’s melanocortin one receptor (MC1R). Activation of this receptor leads to increased production of melanin, which gives the skin a tan appearance. The increased melanin also protects the skin from damage caused by ultraviolet (UV) radiation. 

Pharmacokinetics 

afamelanotide, a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH) used to treat erythropoietic protoporphyria (EPP).  

Absorption 

The absorption of afamelanotide after subcutaneous administration is slow, with a peak plasma concentration of 3.7 ng/mL reached after 36 hours. The area under the curve (AUC) is 42.6 hr⋅ng/mL. 

Distribution 

The volume of distribution, which measures how widely the drug is distributed throughout the body, was found to be about 3 L/kg. 

Metabolism 

afamelanotide is thought to be metabolized and eliminated primarily by the liver, although the exact metabolism of the drug is not fully characterized. It may undergo hydrolysis. The half-life of afamelanotide is 15 hours. 

Elimination/Excretion 

afamelanotide appears to have a rapid onset of action and is eliminated from the body relatively quickly 

Adminstartion

It is essential to follow these instructions carefully when preparing and administering afamelanotide implants. It is also essential to use sterile technique and aseptic precautions throughout the process to minimize the risk of infection. 

It is recommended to allow the implant to warm up to room temperature before use, as this can make it easier to handle. The implant should be removed from the vial using a sterile technique and placed on a sterile surface. 

The insertion site should be identified, and the skin disinfected before administering the implant. Using a local anesthetic is optional but may be considered if the patient is concerned about discomfort. 

The cannula should be inserted into the skin’s subcutaneous (SC) layer at a 30–45-degree angle. The stylet (obturator) should be removed, and the implant loaded into the cannula. The implant should then be gently pushed down the length of the cannula using the stylet. 

After the implant has been inserted, it is essential to verify that it is correctly placed and that no implant or implant portion remains in the cannula. The insertion site should then be covered with a dressing, and the patient should be monitored for at least 30 minutes after implantation. 

afamelanotide implants should be stored in the refrigerator at a temperature between 2-8°C (36-46°F) and protected from light. It is essential to follow the storage instructions carefully to ensure that the implants are effective and safe to use 

Patient Information Leaflet

Patient information leaflet 

Generic Name: afamelanotide 

Pronounced: [ A-fa-me-LAN-oh-tide] 

Why do we use afamelanotide? 

afamelanotide is a synthetic hormone used to treat skin conditions such as erythropoietic protoporphyria (EPP) and solar urticaria. 

In EPP, afamelanotide is used to reduce the skin’s sensitivity to light and prevent attacks of pain and swelling. EPP is a rare inherited disorder that affects the production of a pigment called protoporphyrin. Protoporphyrin is highly sensitive to light, and exposure to sunlight or other light sources can cause severe pain and swell in the skin of people with EPP. afamelanotide helps reduce the skin’s sensitivity to light and reduces the frequency and severity of attacks. 

In solar urticaria, afamelanotide protects the skin from UV-induced hives. Solar urticaria is a rare condition in which the skin becomes sensitive to UV radiation and develops hives or welts in response to sun exposure. afamelanotide helps to protect the skin from UV radiation and reduces the risk of developing hives or welts.