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HIV/AIDS
Tesamorelin
Другие языки:

Tesamorelin

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Tesamorelin
Tesamorelin.svg
Clinical data
Trade names Egrifta SV
AHFS/Drugs.com Multum Consumer Information
MedlinePlus a611035
Routes of
administration		 Subcutaneous injection
ATC code
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability ≤4%
Metabolism Proteolysis
Elimination half-life 26–38 min
Excretion Renal/proteolysis
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
Formula C221H366N72O67S
Molar mass 5135.86 g·mol−1
3D model (JSmol)
  • CCC[C@@H](C(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(cc1)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc3ccc(cc3)O)NC(=O)C/C=C/CC
  • InChI=1S/C220H364N72O67S/c1-24-28-30-54-162(307)259-144(92-119-55-59-121(298)60-56-119)197(342)254-115(20)178(323)275-149(96-168(315)316)198(343)255-116(21)179(324)290-171(110(15)26-3)213(358)283-146(91-118-44-31-29-32-45-118)205(350)292-173(117(22)297)214(359)284-148(95-161(229)306)204(349)288-154(104-296)209(354)279-145(93-120-57-61-122(299)62-58-120)202(347)267-130(52-41-84-247-219(239)240)186(331)266-126(47-34-36-79-222)196(341)289-170(109(13)14)211(356)282-140(87-105(5)6)182(327)251-100-165(310)257-133(64-71-156(224)301)189(334)277-143(90-108(11)12)201(346)287-151(101-293)207(352)256-114(19)177(322)263-129(51-40-83-246-218(237)238)185(330)265-125(46-33-35-78-221)188(333)276-142(89-107(9)10)200(345)278-141(88-106(7)8)199(344)272-137(67-74-159(227)304)194(339)281-150(97-169(317)318)206(351)291-172(111(16)27-4)212(357)274-139(77-86-360-23)195(340)286-152(102-294)208(353)268-131(53-42-85-248-220(241)242)187(332)270-135(65-72-157(225)302)191(336)269-132(63-70-155(223)300)181(326)250-99-164(309)258-134(68-75-166(311)312)190(335)285-153(103-295)210(355)280-147(94-160(228)305)203(348)273-136(66-73-158(226)303)192(337)271-138(69-76-167(313)314)193(338)264-124(48-37-80-243-215(231)232)180(325)249-98-163(308)252-112(17)175(320)261-127(49-38-81-244-216(233)234)183(328)253-113(18)176(321)262-128(50-39-82-245-217(235)236)184(329)260-123(43-25-2)174(230)319/h28-32,44-45,55-62,105-117,123-154,170-173,293-299H,24-27,33-43,46-54,63-104,221-222H2,1-23H3,(H2,223,300)(H2,224,301)(H2,225,302)(H2,226,303)(H2,227,304)(H2,228,305)(H2,229,306)(H2,230,319)(H,249,325)(H,250,326)(H,251,327)(H,252,308)(H,253,328)(H,254,342)(H,255,343)(H,256,352)(H,257,310)(H,258,309)(H,259,307)(H,260,329)(H,261,320)(H,262,321)(H,263,322)(H,264,338)(H,265,330)(H,266,331)(H,267,347)(H,268,353)(H,269,336)(H,270,332)(H,271,337)(H,272,344)(H,273,348)(H,274,357)(H,275,323)(H,276,333)(H,277,334)(H,278,345)(H,279,354)(H,280,355)(H,281,339)(H,282,356)(H,283,358)(H,284,359)(H,285,335)(H,286,340)(H,287,346)(H,288,349)(H,289,341)(H,290,324)(H,291,351)(H,292,350)(H,311,312)(H,313,314)(H,315,316)(H,317,318)(H4,231,232,243)(H4,233,234,244)(H4,235,236,245)(H4,237,238,246)(H4,239,240,247)(H4,241,242,248)/b30-28+/t110-,111-,112-,113-,114-,115-,116-,117+,123-,124-,125-,126-,127+,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,170-,171-,172-,173-/m0/s1
  • Key:VQFDKKWXORFBDI-VAVVJCQZSA-N

Tesamorelin (INN) (trade name Egrifta SV) is a synthetic form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of HIV-associated lipodystrophy, approved initially in 2010. It is produced and developed by Theratechnologies, Inc. of Canada. The drug is a synthetic peptide consisting of all 44 amino acids of human GHRH with the addition of a trans-3-hexenoic acid group.

Mechanism of action

Tesamorelin is the N-terminally modified compound based on 44 amino acids sequence of human GHRH. This modified synthetic form is more potent and stable than the natural peptide. It is also more resistant to cleavage by the dipeptidyl aminopeptidase than human GHRH. It stimulates the synthesis and release of endogenous GH, with an increase in level of insulin-like growth factor (IGF-1). The released GH then binds with the receptors present on various body organs and regulates the body composition. This regulation is mainly because of the combination of anabolic and lipolytic mechanisms. However, it has been found that the main mechanisms by which Tesamorelin reduces body fat mass are lipolysis followed by reduction in triglycerides level.

Contraindication

Tesamorelin therapy may cause glucose intolerance and increase the risk of type 2-diabetes, so it is contraindicated in pregnancy. It is also contraindicated in pregnancy (category X) because it may cause harm to fetus. It is also contraindicated in patients affected by hypothalamic-pituitary axis disruption due to pituitary gland tumor, head irradiation and hypopituitarism.

Adverse effects

Injection site erythema, peripheral edema, injection site pruritus and diarrhea.

See also


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