Investigational Drug Details

Drug ID: D363
Drug Name: Tesamorelin
Synonyms: GHRH(1-44); N-[(3E)-1-oxo-3-hexenyl]Somatoliberin (human pancreatic islet); Tesamorelin
Type: Chemical drug
DrugBank ID: DB08869
DrugBank Description: Tesamorelin is a stabilized synthetic peptide analogue of the hypothalamic peptide, Growth Hormone Releasing Hormone (GHRH) indicated for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Lipodystrophy is a metabolic condition characterized by insulin resistance, fat redistribution, and hyperlipidemia associated with antiretroviral therapy for HIV infection.
PubChem ID: 16137828
CasNo: 218949-48-5
Repositioning for NAFLD: Yes
SMILES: S(CC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)C/C=C/CC)Cc1ccc(O)cc1)C)CC(=O)O)C)[C@H](CC)C)Cc1ccccc1)[C@H](O)C)CC(=O)N)CO)Cc1ccc(O)cc1)CCCNC(=N)N)CCCCN)C(C)C)CC(C)C)CCC(=O)N)CC(C)C)CO)C)CCCNC(=N)N)CCCCN)CC(C)C)CC(C)C)CCC(=O)N)CC(=O)O)[C@H](CC)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N)C)C)CC(=O)N)CO)CO)C
Structure:
InChiKey: QBEPNUQJQWDYKU-BMGKTWPMSA-N
Molecular Weight: 5135.863
DrugBank Targets: Growth hormone-releasing hormone receptor binder
DrugBank MoA: By acting on the pituitary cells in the brain, tesamorelin stimulates production and release of the endogenous hormone (hGRF). Tesamorelin therapy predisposes the patient to glucose intolerance and can also increase the risk of type 2 diabetes, so the drug is contraindicated in pregnancy.
DrugBank Pharmacology: Tesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.
DrugBank Indication: Tesamorelin acetate is a synthetic analogue of human hypothalamic Growth Hormone Releasing Factor (hGRF) indicated to induce and maintain a reduction of excess abdominal fat in HIV-infected patients with lipodystrophy.
Targets: GHRHR agonist;GHRHR binder
Therapeutic Category: Growth stimulant
Clinical Trial Progress: Phase 2 on-going (NCT03375788)
Latest Progress: Under clinical trials

Trial ID Source ID Phases Status Study Results Start Date Last Update Posted
L0085 NCT03375788 Phase 2 Recruiting No Results Available January 17, 2019 March 30, 2021 Details
L0159 NCT02196831 Not applicable Completed Has Results July 1, 2015 January 27, 2020 Details

Target ID Target Name GENE Action Class UniProtKB ID Entry Name

Strategy ID Strategy Synonyms Related Targets Related Drugs
S01 Improve insulin resistance insulin sensitizer; insulin resistance; glucose tolerance Biguanide: increases 5-AMP activated protein kinase signaling; SGLT-2 inhibitor; Thiazalidinedione: selective PPAR-γ agonists; GLP-1 agonist Metformin; Empagliflozin; Canagliflozin; Rosiglitazone; Pioglitazone; Liraglutide Details

Article ID PMID Source Title
A01853 34588764 Drug Des Devel Ther Non-Alcoholic Steatohepatitis (NASH) - A Review of a Crowded Clinical Landscape, Driven by a Complex Disease. Details
A03421 34006921 Sci Rep Delineating tesamorelin response pathways in HIV-associated NAFLD using a targeted proteomic and transcriptomic approach. Details
A03837 33852720 Clin Infect Dis Growth Hormone Releasing Hormone Reduces Circulating Markers of Immune Activation in Parallel with Effects on Hepatic Immune Pathways in Individuals with HIV-infection and Nonalcoholic Fatty Liver Disease. Details
A06908 32701508 JCI Insight Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD. Details
A08045 32270862 Clin Infect Dis Clinical Predictors of Liver Fibrosis Presence and Progression in Human Immunodeficiency Virus-Associated Nonalcoholic Fatty Liver Disease. Details
A09783 31611038 Lancet HIV Effects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. Details
A43477 31611037 Lancet HIV Tesamorelin, liver fat, and NAFLD in the setting of HIV. Details