Identification

Name
Somapacitan
Accession Number
DB15093
Description

Somapacitan, also known as NNC0195-0092,3 is a growth hormone analog indicated to treat adults with growth hormone deficiency.2,6 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.5

Somapacitan was granted FDA approval on 28 August 2020.7

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Protein Chemical Formula
C1038H1609N273O319S9
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Somapacitan
  • Somapacitan (genetical recombination)
  • somapacitan-beco
External IDs
  • NN-8640
  • NN8640
  • NNC-0195-0092
  • NNC0195-0092

Pharmacology

Indication

Somapacitan is indicated as a replacement for growth hormone in adult patients with growth hormone deficiency.6

Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Somapacitan stimulates the growth hormone receptor.6 Somapacitan has a long duration of action as it is given once weekly.6 It has a moderately wide therapeutic window as an acute overdose may cause hypoglycemia followed by hyperglycemia.6 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.6

Mechanism of action

Somapacitan binds to the growth hormone receptor and induces intracellular signalling to up-regulate insulin-like growth factor I (IGF-1).1,6 IGF-1 causes growth in bones and muscle tissue.1 Growth hormones more directly cause the fusion of myoblasts and myotubes to cause muscle fibre growth, activate neural stem cells, and induce chondrocyte proliferation.1

TargetActionsOrganism
UGrowth hormone receptor
agonist
Humans
Absorption

A 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*h/mL.3 A 0.04mg/kg single dose of somapacitan reaches a Cmax of 19.8 ng/mL, with a Tmax of 25.6 hours, and an AUC of 777 ng*h/mL.3 A 0.08mg/kg single dose of somapacitan reaches a Cmax of 64.2 ng/mL, with a Tmax of 16.6 hours, and an AUC of 2753 ng*h/mL.3 A 0.12mg/kg single dose of somapacitan reaches a Cmax of 142.5 ng/mL, with a Tmax of 22.5 hours, and an AUC of 6382 ng*h/mL.3

Volume of distribution

The approximate volume of distribution of somapacitan is 14.6 L.6

Protein binding

Somapacitan is >99% bound to albumin.1,6

Metabolism

Studies in humans and rats show that somapacitan is metabolized through cleavage of the albumin-binding moiety and linker sidechain before further non-specific mechanisms.1,6

Route of elimination

Somapacitan is approximately 81% eliminated in the urine and 13% in the feces.6

Half-life

The elimination half life of somapacitan is 2-3 days.6

Clearance

The apparent maximum rate of saturable elimination is estimated to be 0.268 ± 0.03 mg/h.2

Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Patients experiencing an acute overdose of somapacitan may present with fluid retention.6 Chronic overdose may resemble gigantism or acromegaly.6 Treat patients with symptomatic and supportive measures to minimize the permanent effects.4

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Somapacitan.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Somapacitan.
AlbiglutideThe therapeutic efficacy of Albiglutide can be decreased when used in combination with Somapacitan.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Somapacitan.
AmcinonideThe serum concentration of the active metabolites of Amcinonide can be decreased when Amcinonide is used in combination with Somapacitan.
Beclomethasone dipropionateThe serum concentration of the active metabolites of Beclomethasone dipropionate can be decreased when Beclomethasone dipropionate is used in combination with Somapacitan.
BetamethasoneThe serum concentration of the active metabolites of Betamethasone can be decreased when Betamethasone is used in combination with Somapacitan.
Betamethasone phosphateThe serum concentration of the active metabolites of Betamethasone phosphate can be decreased when Betamethasone phosphate is used in combination with Somapacitan.
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Somapacitan.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Somapacitan.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
No interactions found.

Products

International/Other Brands
Sogroya (Novo Nordisk)

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
8FOJ430U94
CAS number
1338578-34-9

References

General References
  1. Petersen M, Gandhi PS, Buchardt J, Alanentalo T, Fels JJ, Johansen NL, Helding-Kvist P, Vad K, Thygesen P: Tissue Distribution and Receptor Activation by Somapacitan, a Long Acting Growth Hormone Derivative. Int J Mol Sci. 2020 Feb 11;21(4). pii: ijms21041181. doi: 10.3390/ijms21041181. [PubMed:32053994]
  2. Juul RV, Rasmussen MH, Agerso H, Overgaard RV: Pharmacokinetics and Pharmacodynamics of Once-Weekly Somapacitan in Children and Adults: Supporting Dosing Rationales with a Model-Based Analysis of Three Phase I Trials. Clin Pharmacokinet. 2019 Jan;58(1):63-75. doi: 10.1007/s40262-018-0662-5. [PubMed:29671202]
  3. Rasmussen MH, Janukonyte J, Klose M, Marina D, Tanvig M, Nielsen LF, Hoybye C, Andersen M, Feldt-Rasmussen U, Christiansen JS: Reversible Albumin-Binding GH Possesses a Potential Once-Weekly Treatment Profile in Adult Growth Hormone Deficiency. J Clin Endocrinol Metab. 2016 Mar;101(3):988-98. doi: 10.1210/jc.2015-1991. Epub 2016 Jan 4. [PubMed:26727076]
  4. Adelman DT, Liebert KJ, Nachtigall LB, Lamerson M, Bakker B: Acromegaly: the disease, its impact on patients, and managing the burden of long-term treatment. Int J Gen Med. 2013;6:31-8. doi: 10.2147/IJGM.S38594. Epub 2013 Jan 18. [PubMed:23359786]
  5. Rasmussen MH, Olsen MW, Alifrangis L, Klim S, Suntum M: A reversible albumin-binding growth hormone derivative is well tolerated and possesses a potential once-weekly treatment profile. J Clin Endocrinol Metab. 2014 Oct;99(10):E1819-29. doi: 10.1210/jc.2014-1702. Epub 2014 Jul 11. [PubMed:25013997]
  6. Novo Nordisk: Sogroya FDA Label [Link]
  7. FDA Approved Drug Products: Sogroya Somapacitan Subcutaneous Injection [Link]
KEGG Drug
D11194
Wikipedia
Somapacitan

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentAdult Onset Growth Hormone Deficiency / Growth Hormone Disorders3
3RecruitingTreatmentGrowth Hormone Deficiency in Children1
2RecruitingTreatmentGrowth Hormone Deficiency in Children / Growth Hormone Disorders1
2RecruitingTreatmentShort Stature Children Born Small for Gestational Age (SGA)1
1CompletedTreatmentAdult Onset Growth Hormone Deficiency / Growth Hormone Deficiency in Children / Growth Hormone Disorders2
1CompletedTreatmentAdult Onset Growth Hormone Deficiency / Growth Hormone Deficiency in Children / Growth Hormone Disorders / Healthy Volunteers1
1CompletedTreatmentAdult Onset Growth Hormone Deficiency / Growth Hormone Disorders1
1CompletedTreatmentGrowth Hormone Deficiency in Children / Growth Hormone Disorders1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers / Human Growth Hormone Deficiency1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Protein kinase binding
Specific Function
Receptor for pituitary gland growth hormone involved in regulating postnatal body growth. On ligand binding, couples to the JAK2/STAT5 pathway (By similarity).The soluble form (GHBP) acts as a rese...
Gene Name
GHR
Uniprot ID
P10912
Uniprot Name
Growth hormone receptor
Molecular Weight
71498.885 Da
References
  1. Petersen M, Gandhi PS, Buchardt J, Alanentalo T, Fels JJ, Johansen NL, Helding-Kvist P, Vad K, Thygesen P: Tissue Distribution and Receptor Activation by Somapacitan, a Long Acting Growth Hormone Derivative. Int J Mol Sci. 2020 Feb 11;21(4). pii: ijms21041181. doi: 10.3390/ijms21041181. [PubMed:32053994]
  2. Novo Nordisk: Sogroya FDA Label [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
11-beta-hydroxysteroid dehydrogenase [nad(p)] activity
Specific Function
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea...
Gene Name
HSD11B1
Uniprot ID
P28845
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 1
Molecular Weight
32400.665 Da
References
  1. Novo Nordisk: Sogroya FDA Label [Link]
Kind
Protein
Organism
Rat
Pharmacological action
Unknown
Actions
Inducer
General Function
This P450 is active in 15-beta-hydroxylation of steroid sulfates.
Specific Function
Arachidonic acid epoxygenase activity
Gene Name
Cyp2c12
Uniprot ID
P11510
Uniprot Name
Cytochrome P450 2C12, female-specific
Molecular Weight
55918.365 Da
References
  1. Mode A, Tollet P, Strom A, Legraverend C, Liddle C, Gustafsson JA: Growth hormone regulation of hepatic cytochrome P450 expression in the rat. Adv Enzyme Regul. 1992;32:255-63. doi: 10.1016/0065-2571(92)90021-q. [PubMed:1496921]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Jurgens G, Lange KH, Reuther LO, Rasmussen BB, Brosen K, Christensen HR: Effect of growth hormone on hepatic cytochrome P450 activity in healthy elderly men. Clin Pharmacol Ther. 2002 Mar;71(3):162-8. doi: 10.1067/mcp.2002.121373. [PubMed:11907490]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Jurgens G, Lange KH, Reuther LO, Rasmussen BB, Brosen K, Christensen HR: Effect of growth hormone on hepatic cytochrome P450 activity in healthy elderly men. Clin Pharmacol Ther. 2002 Mar;71(3):162-8. doi: 10.1067/mcp.2002.121373. [PubMed:11907490]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Petersen M, Gandhi PS, Buchardt J, Alanentalo T, Fels JJ, Johansen NL, Helding-Kvist P, Vad K, Thygesen P: Tissue Distribution and Receptor Activation by Somapacitan, a Long Acting Growth Hormone Derivative. Int J Mol Sci. 2020 Feb 11;21(4). pii: ijms21041181. doi: 10.3390/ijms21041181. [PubMed:32053994]
  2. Novo Nordisk: Sogroya FDA Label [Link]

Drug created on May 20, 2019 08:49 / Updated on September 03, 2020 14:54

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