tesamorelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
growth hormone release-stimulating peptides	4170	218949-48-5

Description:

Molecule	Description
Synonyms: tesamorelin egrifta tesamorelin acetate	Growth Hormone-Releasing Factor (GRF), also known as growth hormone-releasing hormone (GHRH), is a hypothalamic peptide that acts on the pituitary somatotroph cells to stimulate the synthesis and pulsatile release of endogenous growth hormone (GH), which is both anabolic and lipolytic. GH exerts its effects by interacting with specific receptors on a variety of target cells, including chondrocytes, osteoblasts, myocytes, hepatocytes, and adipocytes, resulting in a host of pharmacodynamic effects. Some, but not all these effects, are primarily mediated by IGF-1 produced in the liver and in peripheral tissues. In vitro, tesamorelin binds and stimulates human GRF receptors with similar potency as the endogenous GRF. Molecular weight: 5040.71 Formula: C215H357N71O67S CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: 2330.50 ALOGS: ROTB: None

Molecule

Description

Synonyms:

tesamorelin
egrifta
tesamorelin acetate

Growth Hormone-Releasing Factor (GRF), also known as growth hormone-releasing hormone (GHRH), is a hypothalamic peptide that acts on the pituitary somatotroph cells to stimulate the synthesis and pulsatile release of endogenous growth hormone (GH), which is both anabolic and lipolytic. GH exerts its effects by interacting with specific receptors on a variety of target cells, including chondrocytes, osteoblasts, myocytes, hepatocytes, and adipocytes, resulting in a host of pharmacodynamic effects. Some, but not all these effects, are primarily mediated by IGF-1 produced in the liver and in peripheral tissues. In vitro, tesamorelin binds and stimulates human GRF receptors with similar potency as the endogenous GRF.

Molecular weight: 5040.71
Formula: C215H357N71O67S
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA: 2330.50
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Nov. 10, 2010	FDA	THERATECHNOLOGIES

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product dose omission issue	223.85	63.63	74	356	119637	34836864
Product administration error	72.66	63.63	20	410	16324	34940177

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product dose omission issue	113.94	48.77	36	165	247501	79496686

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	H01AC06	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES ANTERIOR PITUITARY LOBE HORMONES AND ANALOGUES Somatropin and somatropin agonists
FDA PE	N0000009327	Increased GHRH Activity
MeSH PA	D006133	Growth Substances
FDA EPC	N0000182144	Growth Hormone Releasing Factor Analog

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Lipodystrophy due to Human immunodeficiency virus infection and antiretroviral therapy	indication	705149003
Diabetes mellitus	contraindication	73211009	DOID:9351
Hypopituitarism	contraindication	74728003	DOID:9406
Hyperglycemia	contraindication	80394007	DOID:4195
Injury of head	contraindication	82271004
Transsphenoidal hypophysectomy	contraindication	171948002
Edema	contraindication	267038008
Pregnancy, function	contraindication	289908002
Primary malignant neoplasm	contraindication	372087000
Respiratory insufficiency	contraindication	409623005
Breastfeeding (mother)	contraindication	413712001
Radiation Therapy of Cranium	contraindication
Postsurgical Complications	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Growth hormone-releasing hormone receptor	GPCR	Q02643	GHRHR_HUMAN	AGONIST				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
4030295	VUID
N0000182253	NUI
D06655	KEGG_DRUG
901758-09-6	SECONDARY_CAS_RN
4030295	VANDF
C1876200	UMLSCUI
CHEBI:63626	CHEBI
CHEMBL1237026	ChEMBL_ID
CHEMBL2111290	ChEMBL_ID
DB08869	DRUGBANK_ID
C479538	MESH_SUPPLEMENTAL_RECORD_UI
6959	IUPHAR_LIGAND_ID
8786	INN_ID
MQG94M5EEO	UNII
16137828	PUBCHEM_CID
1044583	RXNORM
178253	MMSL
27618	MMSL
31357	MMSL
d07715	MMSL
013567	NDDF
013568	NDDF
448805009	SNOMEDCT_US
765123002	SNOMEDCT_US
785904004	SNOMEDCT_US

Pharmaceutical products:

None