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15742 details
Primary information
ID15742
Therapeutic IDTh1622
Protein NameSomapacitan
Sequence>Th1622_Somapacitan FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSCVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
Molecular WeightNA
Chemical FormulaC1038H1609N273O319S9
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeThe elimination half life of somapacitan is 2-3 days.[L15661]
DescriptionSomapacitan, also known as NNC0195-0092,[A219136] is a growth hormone analog indicated to treat adults with growth hormone deficiency.[A219126,L15661] This human growth hormone analog differs by the creation of an albumin binding site, and prolonging the effect so that it requires weekly dosing rather than daily.[A219146] Somapacitan was granted FDA approval on 28 August 2020.[L15666]
Indication/DiseaseSomapacitan is indicated as a replacement for growth hormone in adult patients with growth hormone deficiency.[L15661]
PharmacodynamicsSomapacitan stimulates the growth hormone receptor.[L15661] Somapacitan has a long duration of action as it is given once weekly.[L15661] It has a moderately wide therapeutic window as an acute overdose may cause hypoglycemia followed by hyperglycemia.[L15661] Patients should be counselled regarding the risk of increased mortality in patients with critical illness, risk of neoplasms, glucose intolerance in diabetes mellitus, intracranial hypertension, hypersensitivity, fluid retention, hypoadrenalism, hypothyroidism, pancreatitis, lipohypertrophy, and lipoatrophy.[L15661]
Mechanism of ActionSomapacitan binds to the growth hormone receptor and induces intracellular signalling to up-regulate insulin-like growth factor I (IGF-1).[A219096,L15661] IGF-1 causes growth in bones and muscle tissue.[A219096] Growth hormones more directly cause the fusion of myoblasts and myotubes to cause muscle fibre growth, activate neural stem cells, and induce chondrocyte proliferation.[A219096]
ToxicityPatients experiencing an acute overdose of somapacitan may present with fluid retention.[L15661] Chronic overdose may resemble gigantism or acromegaly.[L15661] Treat patients with symptomatic and supportive measures to minimize the permanent effects.[A219141]
MetabolismStudies in humans and rats show that somapacitan is metabolized through cleavage of the albumin-binding moiety and linker sidechain before further non-specific mechanisms.[A219096,L15661]
AbsorptionA 0.02mg/kg single dose of somapacitan reaches a Cmax of 14.4 ng/mL, with a Tmax of 11.1 hours, and an AUC of 475 ng
The approximate volume of distribution of somapacitan is 14.6 L.[L15661]
ClearanceThe apparent maximum rate of saturable elimination is estimated to be 0.268 ± 0.03 mg/h.[A219126]
CategoriesLipids
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetGrowth hormone receptor
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
Contraindication(2S)-5-[2-[2-[2-[[(2S)-1-amino-6-[[2-[(2R)-2-amino-2-carboxyethyl]sulfanylacetyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-[[(4S)-4-carboxy-4-[[2-[2-[2-[4-[16-(2H-tetrazol-5-yl)hexadecanoylsulfamoyl]butanoylamino]ethoxy]ethoxy]acetyl]amino]butanoyl]amino]-5-oxopentanoic acid
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA