Abaloparatide

Abaloparatide
Clinical data
Other names	BA058, BIM-44058
Routes of; administration	Subcutaneous injection
ATC code	none;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name L-alanyl-L-valyl-L-seryl-L-α-glutamyl-L-histidyl-L-glutaminyl-L-leucyl-L-leucyl-L-histidyl-L-α-aspartyl-L-lysylglycyl-L-lysyl-L-seryl-L-isoleucyl-L-glutaminyl-L-α-aspartyl-L-leucyl-L-arginyl-L-arginyl-L-arginyl-L-α-glutamyl-L-leucyl-L-leucyl-L-α-glutamyl-L-lysyl-L-leucyl-L-leucyl-2-methylalanyl-L-lysyl-L-leucyl-L-histidyl-L-threonyl-L-alaninamide;
CAS Number	247062-33-5;
PubChem CID	76943386;
ChemSpider	34443170;
UNII	AVK0I6HY2U;
Chemical and physical data
Formula	C174H299N56O49
Molar mass	3959.649 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)N;
	InChI InChI=1S/C174H300N56O49/c1-26-93(20)136(228-165(274)126(80-232)224-141(250)101(39-28-32-56-176)200-129(236)78-195-140(249)100(38-27-31-55-175)201-161(270)123(73-133(243)244)223-160(269)121(71-98-76-190-82-197-98)220-158(267)118(68-90(14)15)216-155(264)114(64-86(6)7)213-148(257)107(45-50-127(180)234)207-159(268)120(70-97-75-189-81-196-97)219-151(260)111(49-54-132(241)242)209-164(273)125(79-231)225-167(276)135(92(18)19)227-139(248)94(21)179)168(277)210-108(46-51-128(181)235)149(258)222-124(74-134(245)246)162(271)217-112(62-84(2)3)152(261)205-105(44-37-61-194-173(187)188)143(252)203-103(42-35-59-192-171(183)184)142(251)204-104(43-36-60-193-172(185)186)144(253)206-110(48-53-131(239)240)150(259)214-115(65-87(8)9)154(263)215-113(63-85(4)5)153(262)208-109(47-52-130(237)238)147(256)202-102(40-29-33-57-177)145(254)211-116(66-88(10)11)156(265)218-119(69-91(16)17)166(275)230-174(24,25)170(279)226-106(41-30-34-58-178)146(255)212-117(67-89(12)13)157(266)221-122(72-99-77-191-83-198-99)163(272)229-137(96(23)233)169(278)199-95(22)138(182)247/h75-77,81-96,100-126,135-137,231-233H,26-74,78-80,175-179H2,1-25H3,(H2,180,234)(H2,181,235)(H2,182,247)(H,189,196)(H,190,197)(H,191,198)(H,195,249)(H,199,278)(H,200,236)(H,201,270)(H,202,256)(H,203,252)(H,204,251)(H,205,261)(H,206,253)(H,207,268)(H,208,262)(H,209,273)(H,210,277)(H,211,254)(H,212,255)(H,213,257)(H,214,259)(H,215,263)(H,216,264)(H,217,271)(H,218,265)(H,219,260)(H,220,267)(H,221,266)(H,222,258)(H,223,269)(H,224,250)(H,225,276)(H,226,279)(H,227,248)(H,228,274)(H,229,272)(H,230,275)(H,237,238)(H,239,240)(H,241,242)(H,243,244)(H,245,246)(H4,183,184,192)(H4,185,186,193)(H4,187,188,194)/t93-,94-,95-,96+,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,135-,136-,137-/m0/s1; Key:BVISQZFBLRSESR-XSCWXTNMSA-N;

Abaloparatide is a parathyroid hormone-related protein (PTHrP) analog drug in development for treating osteoporosis.^[1] Like the related drug teriparatide, and unlike bisphosphonates, it is an anabolic (i.e., bone growing) agent.^[2]

A subcutaneous injection formulation of the drug has completed a Phase III trial for osteoporosis.^[3] This single study found a decrease in fractures.^[4] A transdermal patch is also in development.^[2]

References

Template:Research help

^ http://www.genengnews.com/gen-news-highlights/radius-raises-26-75m-for-phase-iii-osteoporosis-trial/81245990/
^ ^a ^b H. Spreitzer (18 January 2016). "Neue Wirkstoffe – Abaloparatid". Österreichische Apothekerzeitung (in German) (2/2016): 12.
^ Clinical trial number NCT01343004 for "Phase III Study to Evaluate the Safety and Efficacy of BA058 for Prevention of Fracture in Postmenopausal Women" at ClinicalTrials.gov
^ Miller, PD; Hattersley, G; Riis, BJ; Williams, GC; Lau, E; Russo, LA; Alexandersen, P; Zerbini, CA; Hu, MY; Harris, AG; Fitzpatrick, LA; Cosman, F; Christiansen, C; ACTIVE Study, Investigators. (16 August 2016). "Effect of Abaloparatide vs Placebo on New Vertebral Fractures in Postmenopausal Women With Osteoporosis: A Randomized Clinical Trial". JAMA. 316 (7): 722–33. PMID 27533157.

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[1] ttp://www.genengnews.com/gen-news-highlights/radius-raises-26-75m-for-phase-iii-osteoporosis-trial/81245990/

[Spreitzer-2] H. Spreitzer (18 January 2016). "Neue Wirkstoffe – Abaloparatid". Österreichische Apothekerzeitung (in German) (2/2016): 12.

[3] Clinical trial number NCT01343004 for "Phase III Study to Evaluate the Safety and Efficacy of BA058 for Prevention of Fracture in Postmenopausal Women" at ClinicalTrials.gov

[4] Miller, PD; Hattersley, G; Riis, BJ; Williams, GC; Lau, E; Russo, LA; Alexandersen, P; Zerbini, CA; Hu, MY; Harris, AG; Fitzpatrick, LA; Cosman, F; Christiansen, C; ACTIVE Study, Investigators. (16 August 2016). "Effect of Abaloparatide vs Placebo on New Vertebral Fractures in Postmenopausal Women With Osteoporosis: A Randomized Clinical Trial". JAMA. 316 (7): 722–33. PMID 27533157.

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