Product Name

Tesamorelin Acetate

CAS Number

901758-09-6

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Product Name:
Tesamorelin Acetate
CAS Number:
901758-09-6
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.
Mode of Action:

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.

Pharmacodynamics:

Tesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.

Metabolism:

No formal metabolism studies have been performed in humans.

Toxicity:

Diarrhea, congestive heart failure, peripheral neuropathy, and loss of mobility were the four serious adverse events reported during the clinical studies

IUPAC:
L-Leucinamide, N-((3E)-1-oxo-3-hexenyl)-L-tyrosyl-L-alanyl-L-alpha-aspartyl-L-alanyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-asparaginyl-L-seryl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucylglycyl-L-glutaminyl-L-leucyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-leucyl-L-glutaminyl-L-alpha-aspartyl-L-isoleucyl-L-methionyl-L-seryl-L-arginyl-L-glutaminyl-L-glutaminylglycyl-L-alpha-glutamyl-L-seryl-L-asparaginyl-L-glutaminyl-L-alpha-glutamyl-L-arginylglycyl-L-alanyl-L-arginyl-L-alanyl-L-arginyl-, acetate (salt)
ATC:
H01AC06
DrugBank:
DB08869
Formula:
C221-H366-N72-O67-S.(C2-H4-O2)x-
Molecular Mass:
5195.877
Synonyms:
(3E)-Hex-3-enoylsomatoliberin (human) acetate (salt), Tesamorelin acetate, TH9507, UNII-LGW5H38VE3
SMILES:
C(=O)(C/C=C/CC)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N)CC(C)C)CCCNC(=N)N)CCCNC(=N)N)CCCNC(=N)N)CCC(=O)O)CCC(=O)N)CC(=O)N)CO)CCC(=O)O)CCC(=O)N)CCC(=O)N)CCCNC(=N)N)CO)CCSC)[C@@H](C)CC)CC(=O)O)CCC(=O)N)CC(C)C)CC(C)C)CCCCN)CCCNC(=N)N)CO)CC(C)C)CCC(=O)N)CC(C)C)[C@@H](C)C)CCCCN)CCCNC(=N)N)Cc1ccc(cc1)O)CO)CC(=O)N)[C@@H](O)C)Cc1ccccc1)[C@@H](C)CC)CC(=O)O)Cc1ccc(cc1)O.CC(=O)O
General Reference:
General Reference:

  1. Spooner LM, Olin JL: Tesamorelin: a growth hormone-releasing factor analogue for HIV-associated lipodystrophy. Ann Pharmacother. 2012 Feb;46(2):240-7. doi: 10.1345/aph.1Q629. Epub 2012 Jan 31. Pubmed
  2. McLarnon A: Neuroendocrinology: Tesamorelin can improve cognitive function. Nat Rev Endocrinol. 2012 Oct;8(10):568. doi: 10.1038/nrendo.2012.151. Epub 2012 Aug 28. Pubmed
  3. Bedimo R: Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl). 2011;3:69-79. doi: 10.2147/HIV.S14561. Epub 2011 Jul 10. Pubmed
  4. Dhillon S: Spotlight on tesamorelin in HIV-associated lipodystrophy. BioDrugs. 2011 Dec 1;25(6):405-8. doi: 10.2165/11208290-000000000-00000. Pubmed
  5. Garg A: Acquired and inherited lipodystrophies. N Engl J Med. 2004 Mar 18;350(12):1220-34. Pubmed
  6. Patel A, Gandhi H, Upaganlawar A: Tesamorelin: A hope for ART-induced lipodystrophy. J Pharm Bioallied Sci. 2011 Apr;3(2):319-20. doi: 10.4103/0975-7406.80763. Pubmed
  7. Campbell RM, Lee Y, Rivier J, Heimer EP, Felix AM, Mowles TF: GRF analogs and fragments: correlation between receptor binding, activity and structure. Peptides. 1991 May-Jun;12(3):569-74. Pubmed

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