Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C78H111N21O19.3C2H4O2 |
Molecular Weight | 1827.0011 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 12 / 12 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)=O.CC(O)=O.CC(O)=O.CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@H](CC3=CC=CC=C3)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC4=CNC5=CC=CC=C45)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N6CCC[C@H]6C(=O)N[C@@H](C(C)C)C(N)=O
InChI
InChIKey=VHLLBJXKNRAYGM-BHHWPIKXSA-N
InChI=1S/C78H111N21O19.3C2H4O2/c1-5-6-19-52(91-75(116)61(41-101)97-72(113)57(34-46-24-26-49(103)27-25-46)94-74(115)60(40-100)88-44(4)102)68(109)92-54(28-29-64(105)106)70(111)96-59(36-48-38-83-42-87-48)73(114)93-56(33-45-16-8-7-9-17-45)71(112)90-53(22-14-31-84-78(81)82)69(110)95-58(35-47-37-85-51-20-11-10-18-50(47)51)67(108)86-39-63(104)89-55(21-12-13-30-79)77(118)99-32-15-23-62(99)76(117)98-65(43(2)3)66(80)107;3*1-2(3)4/h7-11,16-18,20,24-27,37-38,42-43,52-62,65,85,100-101,103H,5-6,12-15,19,21-23,28-36,39-41,79H2,1-4H3,(H2,80,107)(H,83,87)(H,86,108)(H,88,102)(H,89,104)(H,90,112)(H,91,116)(H,92,109)(H,93,114)(H,94,115)(H,95,110)(H,96,111)(H,97,113)(H,98,117)(H,105,106)(H4,81,82,84);3*1H3,(H,3,4)/t52-,53-,54-,55-,56+,57-,58-,59-,60-,61-,62-,65-;;;/m0.../s1
Molecular Formula | C78H111N21O19 |
Molecular Weight | 1646.8452 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 12 / 12 |
E/Z Centers | 6 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C2H4O2 |
Molecular Weight | 60.052 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Afamelanotide (SCENESSE) is a synthetic α-melanocyte stimulating hormone analog and first-in-class melanocortin-1 receptor agonist that is approved in the EU for the prevention of phototoxicity in adults with erythropoietic protoporphyria. Afamelanotide differs from endogenous α-melanocyte stimulating hormone at the fourth and seventh amino acid residues, increasing its resistance to immediate degradation and increasing its binding time to melanocortin-1 receptor. Afamelanotide is mimic the pharmacological activity of α-melanocyte stimulating hormone by binding to the melanocortin-1 receptor on melanocytes and activating the synthesis of eumelanin. Eumelanin provides photoprotection through mechanisms including, but not limited to, the absorption and scattering of visible and UV light and antioxidant activity. Afamelanotide increases eumelanin density in healthy volunteers and patients with erythropoietic protoporphyria. In healthy, fair-skinned volunteers, a significant increase in melanin density and skin darkening in both sun-exposed and non-sun-exposed sites was seen with subcutaneous injections of afamelanotide. The most common afamelanotide adverse events included headache and nausea. Common adverse effects include back pain, upper respiratory tract infections, decreased appetite, migraine, and dizziness.
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.7 ng/mL |
16 mg single, subcutaneous dose: 16 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
AFAMELANOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
138.9 ng × h/mL |
16 mg single, subcutaneous dose: 16 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
AFAMELANOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
15 h |
16 mg single, subcutaneous dose: 16 mg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
AFAMELANOTIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Other AEs: Implant site reaction, Nausea... Other AEs: Implant site reaction (grade 1-2, 21%) Sources: Nausea (grade 1-2, 19%) Oropharyngeal pain (grade 1-2, 7%) Cough (grade 1-2, 6%) Fatigue (grade 1-2, 6%) Skin hyperpigmentation (grade 1-2, 4%) Dizziness (grade 1-2, 4%) Melanocytic nevus (grade 1-2, 4%) Respiratory tract infection (grade 1-2, 4%) Somnolence (grade 1-2, 2%) Porphyria non-acute (grade 1-2, 2%) Skin irritation (grade 1-2, 2%) Implant site discoloration (grade 1-2, 10%) |
16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Other AEs: Abdominal pain, Upper abdominal pain... Other AEs: Abdominal pain (grade 1-2, 11%) Sources: Upper abdominal pain (grade 1-2, 3%) Diarrhea (grade 1-2, 8%) Vomiting (grade 1-2, 3%) Fatigue (grade 1-2, 3%) Implant site discoloration (grade 1-2, 19%) Viral gastroenteritis (grade 1-2, 3%) Influenza (grade 1-2, 16%) Nasopharyngitis (grade 1-2, 21%) Upper respiratory tract infection (grade 1-2, 8%) Blood in urine (grade 1-2, 5%) Back pain (grade 1-2, 5%) Myalgia (grade 1-2, 3%) Pain in extremity (grade 1-2, 3%) Headache (grade 1-3, 34%) Migraine (grade 1-2, 3%) Cough (grade 1-2, 13%) Oropharyngeal pain (grade 1-2, 16%) Eczema (grade 1-2, 5%) Pigmentation disorder (grade 1-2, 8%) Pruritus (grade 1-2, 5%) Nausea (grade 1-2, 18%) |
16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Other AEs: Abdominal discomfort, Abdominal pain... Other AEs: Abdominal discomfort (grade 1-2, 2%) Sources: Abdominal pain (grade 1-2, 2%) Upper abdominal pain (grade 1-2, 2%) Diarrhea (grade 1-2, 4%) Dyspepsia (grade 1-2, 6%) Toothache (grade 1-2, 6%) Vomiting (grade 1-2, 2%) Implant site discoloration (grade 1-2, 11%) Pain (grade 1-2, 8%) Influenza (grade 1-2, 4%) Nasopharyngitis (grade 1-2, 12%) Sinusitis (grade 1-2, 6%) Upper respiratory tract infection (grade 1-2, 2%) Arthralgia (grade 1-2, 10%) Back pain (grade 1-2, 12%) Musculoskeletal pain (grade 1-2, 6%) Myalgia (grade 1-2, 6%) Pain in extremity (grade 1-2, 4%) Dizziness (grade 1-2, 2%) Headache (grade 1-2, 40%) Migraine (grade 1-2, 6%) Sinus headache (grade 1-2, 2%) Cough (grade 1-2, 2%) Oropharyngeal pain (grade 1-2, 4%) Pigmentation disorder (grade 1-2, 2%) Pruritus (grade 1-2, 4%) Melanocytic nevus (grade 1-2, 4%) Nausea (grade 1-2, 19%) |
0.16 mg/kg 10 times / month multiple, subcutaneous MTD Dose: 0.16 mg/kg, 10 times / month Route: subcutaneous Route: multiple Dose: 0.16 mg/kg, 10 times / month Sources: |
healthy, adult Health Status: healthy Age Group: adult Sources: |
Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea Sources: |
18 mg 1 times / 60 days multiple, subcutaneous (mean) Studied dose Dose: 18 mg, 1 times / 60 days Route: subcutaneous Route: multiple Dose: 18 mg, 1 times / 60 days Sources: |
unhealthy, adult n = 36 Health Status: unhealthy Condition: Polymorphous Light Eruption Age Group: adult Sex: M+F Population Size: 36 Sources: |
Disc. AE: Crohn's disease... AEs leading to discontinuation/dose reduction: Crohn's disease Sources: |
20 mg 1 times / 2 months multiple, subcutaneous Highest studied dose Dose: 20 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 20 mg, 1 times / 2 months Sources: |
unhealthy n = 43 Health Status: unhealthy Condition: organ transplant recipients Population Size: 43 Sources: |
|
40 mg 1 times / day single, subcutaneous Highest studied dose Dose: 40 mg, 1 times / day Route: subcutaneous Route: single Dose: 40 mg, 1 times / day Sources: |
healthy n = 6 Health Status: healthy Population Size: 6 Sources: |
Disc. AE: Darkened skin... AEs leading to discontinuation/dose reduction: Darkened skin Sources: |
16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy n = 74 Health Status: unhealthy Condition: erythropoietic protoporphyria Population Size: 74 Sources: |
Disc. AE: Migraine... AEs leading to discontinuation/dose reduction: Migraine Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Implant site discoloration | grade 1-2, 10% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Nausea | grade 1-2, 19% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Porphyria non-acute | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Skin irritation | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Somnolence | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Implant site reaction | grade 1-2, 21% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Dizziness | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Melanocytic nevus | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Respiratory tract infection | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Skin hyperpigmentation | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Cough | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Fatigue | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Oropharyngeal pain | grade 1-2, 7% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 18 to 74 years n = 125 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 18 to 74 years Sex: M+F Population Size: 125 Sources: |
Abdominal pain | grade 1-2, 11% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Cough | grade 1-2, 13% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Influenza | grade 1-2, 16% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Oropharyngeal pain | grade 1-2, 16% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Nausea | grade 1-2, 18% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Implant site discoloration | grade 1-2, 19% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Nasopharyngitis | grade 1-2, 21% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Fatigue | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Migraine | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Myalgia | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Pain in extremity | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Upper abdominal pain | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Viral gastroenteritis | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Vomiting | grade 1-2, 3% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Back pain | grade 1-2, 5% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Blood in urine | grade 1-2, 5% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Eczema | grade 1-2, 5% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Pruritus | grade 1-2, 5% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Diarrhea | grade 1-2, 8% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Pigmentation disorder | grade 1-2, 8% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Upper respiratory tract infection | grade 1-2, 8% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Headache | grade 1-3, 34% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 38.3 n = 38 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 38.3 Sex: M+F Population Size: 38 Sources: |
Arthralgia | grade 1-2, 10% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Implant site discoloration | grade 1-2, 11% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Back pain | grade 1-2, 12% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Nasopharyngitis | grade 1-2, 12% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Nausea | grade 1-2, 19% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Abdominal discomfort | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Abdominal pain | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Cough | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Dizziness | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Pigmentation disorder | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Sinus headache | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Upper abdominal pain | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Upper respiratory tract infection | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Vomiting | grade 1-2, 2% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Diarrhea | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Influenza | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Melanocytic nevus | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Oropharyngeal pain | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Pain in extremity | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Pruritus | grade 1-2, 4% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Headache | grade 1-2, 40% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Dyspepsia | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Migraine | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Musculoskeletal pain | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Myalgia | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Sinusitis | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Toothache | grade 1-2, 6% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Pain | grade 1-2, 8% | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy, 40.4 n = 48 Health Status: unhealthy Condition: erythropoietic protoporphyria Age Group: 40.4 Sex: M+F Population Size: 48 Sources: |
Nausea | Disc. AE | 0.16 mg/kg 10 times / month multiple, subcutaneous MTD Dose: 0.16 mg/kg, 10 times / month Route: subcutaneous Route: multiple Dose: 0.16 mg/kg, 10 times / month Sources: |
healthy, adult Health Status: healthy Age Group: adult Sources: |
Crohn's disease | Disc. AE | 18 mg 1 times / 60 days multiple, subcutaneous (mean) Studied dose Dose: 18 mg, 1 times / 60 days Route: subcutaneous Route: multiple Dose: 18 mg, 1 times / 60 days Sources: |
unhealthy, adult n = 36 Health Status: unhealthy Condition: Polymorphous Light Eruption Age Group: adult Sex: M+F Population Size: 36 Sources: |
Darkened skin | Disc. AE | 40 mg 1 times / day single, subcutaneous Highest studied dose Dose: 40 mg, 1 times / day Route: subcutaneous Route: single Dose: 40 mg, 1 times / day Sources: |
healthy n = 6 Health Status: healthy Population Size: 6 Sources: |
Migraine | Disc. AE | 16 mg 1 times / 2 months multiple, subcutaneous Recommended Dose: 16 mg, 1 times / 2 months Route: subcutaneous Route: multiple Dose: 16 mg, 1 times / 2 months Sources: |
unhealthy n = 74 Health Status: unhealthy Condition: erythropoietic protoporphyria Population Size: 74 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210797Orig1s000OtherR.pdf#page=70 Page: 70.0 |
unlikely | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210797Orig1s000OtherR.pdf#page=70 Page: 70.0 |
unlikely |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210797Orig1s000OtherR.pdf#page=69 Page: 35.0 |
PubMed
Title | Date | PubMed |
---|---|---|
4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity. | 1980 Oct |
|
Skin pigmentation and pharmacokinetics of melanotan-I in humans. | 1997 Apr |
|
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat. | 1999 Aug 13 |
|
Pharmacologic response of a controlled-release PLGA formulation for the alpha-melanocyte stimulating hormone analog, Melanotan-I. | 2000 May |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26979527
Afamelanotide is supplied in a biodegradable, controlled-release implant containing 16 mg of the active drug, which is to be administered subcutaneously in the area above the suprailiac crest using a 14-gauge catheter with needle
Route of Administration:
Other
Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 05:01:03 GMT 2023
by
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Sat Dec 16 05:01:03 GMT 2023
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Record UNII |
1XCC161YKC
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Validated (UNII)
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EU-Orphan Drug |
EU/3/08/541
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2278002
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1566590-77-9
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NON-SPECIFIC STOICHIOMETRY | |||
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C166521
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EF-158
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136034
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1XCC161YKC
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133083079
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PRIMARY |
Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
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ACTIVE MOIETY |