Tesamorelin

Tesamorelin
Clinical data

Trade names	Egrifta
AHFS/Drugs.com	Multum Consumer Information
MedlinePlus	a611035
Pregnancy category	US: X (Contraindicated)
Routes of administration	Subcutaneous injection
ATC code	H01AC06 (WHO)
Legal status
Legal status	US: ℞-only ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	≤4%^[1]
Metabolism	Proteolysis
Biological half-life	26–38 min
Excretion	Renal/proteolysis
Identifiers
CAS Number	901758-09-6^Y
PubChem (CID)	16137828
ChemSpider	34982925
UNII	MQG94M5EEO^Y
KEGG	D09015^Y
Chemical and physical data
Formula	C₂₂₁H₃₆₆N₇₂O₆₇S
Molar mass	5135.86 g/mol
3D model (Jmol)	Interactive image
SMILES 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 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) is a synthetic form of growth-hormone-releasing hormone (GHRH) which is used in the treatment of HIV-associated lipodystrophy. 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.^[2]

References

↑ "Egrifta (tesamorelin for injection) for Subcutaneous Use. U.S. Full Prescribing Information" (PDF). EMD Serono, Inc. Retrieved 9 April 2016.
↑ "FDA Application Chemistry Review" (PDF).

Protein and peptide receptor modulators

Adiponectin

AdipoR₁	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon (–)-Arctigenin Arctiin Gramine Matairesinol Antagonists: Peptide: ADP-400

AdipoR₂	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon Deoxyschizandrin Parthenolide Syringing Taxifoliol Antagonists: Peptide: ADP-400

Angiotensin

Agonists: Angiotensin II
Angiotensin III
Angiotensin IV
Saralasin

Antagonists: Abitesartan
Azilsartan
Azilsartan medoxomil
Candesartan
Elisartan
Embusartan
Eprosartan
EXP-3174
Fimasartan
Forasartan
Irbesartan
Losartan
Milfasartan
Olmesartan
Olmesartan medoxomil
PD123319
Pomisartan
Pratosartan
Ripisartan
Saprisartan
Sparsentan
Tasosartan
Telmisartan
Valsartan
Zolasartan

Renin inhibitors: Aliskiren
Ciprokiren
Ditekiren
Enalkiren
Pepstatin
Remikiren
Terlakiren
Zankiren

Propeptides: Angiotensinogen
Angiotensin I

Bradykinin

Agonists: Bradykinin
Kallidin

Antagonists: FR-173657
Icatibant
LF22-0542

CGRP

Agonists: Amylin
CGRP
Pramlintide

Antagonists: BI 44370 TA
BMS-927711
CGRP (8-37)
MK-3207
Olcegepant
Rimegepant
SB-268262
Telcagepant
Ubrogepant

Antibodies: ALD403
Eptinezumab
Erenumab
Fremanezumab

Cholecystokinin

CCK_A	Agonists: Cholecystokinin Antagonists: Amiglumide Asperlicin Devazepide Dexloxiglumide Lintitript Lorglumide Loxiglumide Pranazepide Proglumide Tarazepide Tomoglumide

CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Pentagastrin (CCK-5) Antagonists: CI-988 (PD-134308) Itriglumide L-365,360 Netazepide Proglumide Spiroglumide

Unsorted	Antagonists: Nastorazepide

CRH

CRF₁	Agonists: Cortagine Corticorelin Corticotropin releasing hormone Sauvagine Stressin I Urocortin Antagonists: Antalarmin Astressin-B CP-154,526 Emicerfont Hypericin LWH-234 NBI-27914 Pexacerfont R-121919 TS-041 Verucerfont

CRF₂	Agonists: Corticorelin Corticotropin releasing hormone Sauvagine Urocortin Antagonists: Astressin-B

Cytokine

See here instead.

Endothelin

Agonists: Endothelin 1
Endothelin 2
Endothelin 3
IRL-1620

Antagonists: A-192621
ACT-132577
Ambrisentan
Atrasentan
Avosentan
Bosentan
BQ-123
BQ-788
Clazosentan
Darusentan
Edonentan
Enrasentan
Fandosentan
Feloprentan
Macitentan
Nebentan
Sitaxentan
Sparsentan
Tezosentan
Zibotentan

Galanin

GAL₁	Agonists: Galanin Galanin (1-15) Galanin-like peptide Galmic Galnon Antagonists: C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH-202596

GAL₂	Agonists: Galanin Galanin (1-15) Galanin (2-11) Galanin-like peptide Galmic Galnon J18 Antagonists: C7 Galantide (M15) M32 M35 M40 M871

GAL₃	Agonists: Galanin Galanin (1-15) Galmic Galnon Antagonists: C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299

Ghrelin/GHS

Agonists: Peptide: Alexamorelin
Cortistatin-14
Examorelin (hexarelin)
Ghrelin
GHRP-1
GHRP-3
GHRP-4
GHRP-5
GHRP-6
Ipamorelin
Lenomorelin
Pralmorelin (GHRP-2)
Relamorelin
Tabimorelin
Ulimorelin; Non-peptide: Adenosine
Anamorelin
Capromorelin
CP-464709
Ibutamoren (MK-677)
L-692,585
Macimorelin
SM-130686; Unsorted: LY-426410
LY-444711

Antagonists: A-778193
Cortistatin-8
(D-Lys³)-GHRP-6
JMV2959
YIL-781

Binding proteins: Growth hormone-binding protein

Agonists: Bovine somatotropin
Efpegsomatropin
Growth hormone
Human placental lactogen
Somagrebove
Somapacitan
Somatosalm
Somatotropin
Somatropin pegol
Somatrem
Sometribove
Somatrogon (MOD-4023; hGH-CTP)
Somavaratan
Somavubove
Somidobove

Antagonists: G120K-hGH
Pegvisomant

GHRH

Agonists: Peptide: CJC-1295
Dumorelin
GHRH
Modified GRF (1-29)
Rismorelin
Sermorelin
Somatorelin
Tesamorelin

Antagonists: MZ-5-156

GLP

GLP-1	Agonists: Albiglutide Dulaglutide Efpeglenatide Exenatide GLP-1 Langlenatide Liraglutide Lixisenatide Oxyntomodulin Semaglutide Taspoglutide

GLP-2	Agonists: Elsiglutide GLP-2 Teduglutide

Others	Propeptides: Preproglucagon Proglucagon

Glucagon

Agonists: Glucagon
Oxyntomodulin

Antagonists: Adomeglivant
L-168,049
LGD-6972

Propeptides: Preproglucagon
Proglucagon

GnRH

Antagonists: Peptide: Abarelix
Acyline
Cetrorelix
Degarelix
Detirelix
Ganirelix
Iturelix
Ozarelix
Prazarelix
Ramorelix
Teverelix (antarelix); Non-peptide: ASP-1707
Elagolix
KLH-2109
Relugolix
Sufugolix

Gonadotropin

LH/CG	Agonists: Choriogonadotropin alfa Human chorionic gonadotropin Luteinizing hormone Lutropin alfa Menotropin (human menopausal gonadotropin)

FSH	Agonists: Corifollitropin alfa Follicle-stimulating hormone Follitropin alfa Follitropin beta Follitropin epsilon Menotropin (human menopausal gonadotropin) Urofollitropin Varfollitropin alfa NAMs: ADX-61623

Growth factor

See here instead.

Insulin

Antagonists: BMS-754807
S661
S961

Kinase inhibitors: Linsitinib

Kisspeptin

Agonists: Kisspeptin
Kisspeptin-10

Antagonists: Kisspeptin-234

Leptin

Agonists: Leptin
Metreleptin

MCH

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0065 ATC-0175 GW-803430 NGD-4715 SNAP-7941 SNAP-94847

MCH₂	Agonists: Melanin concentrating hormone

Melanocortin

See here instead.

Neuropeptide FF

Agonists: Neuropeptide AF
Neuropeptide FF
Neuropeptide SF (RFRP-1)
Neuropeptide VF (RFRP-3)

Antagonists: BIBP-3226
RF9

Neuropeptide S

Agonists: Neuropeptide S

Antagonists: ML-154
SHA-68

Neuropeptide Y

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBO-3304 BIBP-3226 BVD-10 GR-231118 PD-160170

Y₂	Agonists: 2-Thiouridine 5'-triphosphate Neuropeptide Y Neuropeptide Y (13-36) Peptide YY Peptide YY (3-36) Antagonists: BIIE-0246 JNJ-5207787 SF-11

Y₄	Agonists: GR-231118 Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49

Y₅	Agonists: BWX-46 Neuropeptide Y Peptide YY Antagonists: CGP-71683 FMS-586 L-152,804 Lu AA-33810 MK-0557 NTNCB Velneperit (S-2367)

Neurotensin

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: Meclinertant SR-142948

NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142948

Opioid

See here instead.

Orexin

OX₁	Agonists: Orexin (A, B) Antagonists: ACT-335827 ACT-462206 Almorexant Filorexant Lemborexant SB-334867 SB-408124 SB-649868 Suvorexant TCS-1102

OX₂	Agonists: Orexin (A, B) SB-668875 Antagonists: ACT-335827 ACT-462206 Almorexant EMPA Filorexant JNJ-10397049 MIN-202 (JNJ-42847922) Lemborexant MK-1064 SB-649868 Suvorexant TCS-1102 TCS-OX2-29

Unsorted	Antagonists: Seltorexant

Oxytocin

See here instead.

Prolactin

Antagonists: Δ1–9-G129R-hPRL
Δ1–14-G129R-hPRL
G120K-hGH
G129R-hPRL

PTH

Agonists: Abaloparatide
Parathyroid hormone
Parathyroid hormone-related protein (PTHrP)
Semparatide
Teriparatide

Relaxin

Somatostatin

Agonists: BIM-23052
CH-275
Cortistatin-14
Depreotide
Ilatreotide
L-803,087
L-817,818
Lanreotide
NNC 26-9100
Octreotide
Pasireotide
Pentetreotide
RC-160
Seglitide
Somatostatin (GHIH)
Somatostatin (1-28)
SRIF-14
SRIF-28
TT-232
Vapreotide

Antagonists: BIM-23056
Cyclosomatostatin
CYN-154806
Satoreotide

Tachykinin

NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant

NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant

NK₃	Agonists: Neurokinin B Antagonists: Fezolinetant Osanetant Talnetant

TRH

Agonists: Azetirelin
Fertirelin
Montirelin
Orotirelin
Posatirelin
Protirelin
Rovatirelin
Taltirelin
TRH (TRF)

TSH

Agonists: Thyrotropin alfa
TSH (thyrotropin)

Vasopressin

See here instead.

VIP/PACAP

VIPR₁	Agonists: Peptide: Bay 55-9837 LBT-3393 PACAP VIP

VIPR₂	Agonists: Peptide: LBT-3627 PACAP VIP

PAC₁	Agonists: PACAP PACAP (1-27) PACAP (1-38) Antagonists: PACAP (6-38)

Unsorted	PHI PHM PHV

Others

Endogenous: Adrenomedullin
Apelin
Bombesin
Calcitonin
Carnosine
CART
CLIP
DSIP
Enteroglucagon
Formyl peptide
GALP
GIP
GRP
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin)
Kininogens
Motilin
Natriuretic peptides (ANP, BNP, CNP, urodilatin)
Nesfatin-1
Neuromedin B
Neuromedin N
Neuromedin S
Neuromedin U
Obestatin
Osteocalcin
Resistin
Secretin
Thymopoietin
Thymosins
Thymulin
Urotensin-II
VGF

Exogenous: Lifitegrast (LFA-1 antagonist)

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Tesamorelin

See also

References