卡格列肽

卡格列肽
臨床資料
其他名稱	GLXC-26801
ATC碼	未分配;
識別資訊
	IUPAC命名法 20-[[(1S)-4-[[(2S)-6-amino-1-[[(4R,7S,10S,13S,16S,19R)-4-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2R)-4-amino-1-[[(2S)-1-[[2-[(2S)-2-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[(2S)-2-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-16-(2-amino-2-oxoethyl)-7,13-bis[(1R)-1-hydroxyethyl]-10-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxohexan-2-yl]amino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid; ;
CAS號	1415456-99-3
PubChem CID	167312356;
DrugBank	DB18887;
ChemSpider	129424923;
UNII	AO43BIF1U8;
化學資訊
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N2CCC[C@H]2C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N3CCC[C@H]3C(=O)N)NC(=O)[C@@H]4CCCN4C(=O)CNC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@@H](CC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CC6=CNC=N6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@@H]8CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N8)[C@@H](C)O)C)[C@@H](C)O)CC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)CC[C@@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O;
	InChI InChI=1S/C194H312N54O59S2/c1-19-100(10)151(184(298)233-128(78-98(6)7)189(303)248-75-49-60-137(248)190(304)247-74-48-59-136(247)182(296)243-155(107(17)255)187(301)232-127(86-143(201)262)173(287)238-150(99(8)9)183(297)210-88-146(265)218-129(90-249)176(290)230-126(85-142(200)261)175(289)244-156(108(18)256)191(305)246-73-46-57-134(246)157(202)271)239-181(295)135-58-47-72-245(135)147(266)89-211-161(275)120(79-109-50-36-34-37-51-109)225-171(285)123(82-139(197)258)228-172(286)124(83-140(198)259)229-177(291)130(91-250)235-178(292)131(92-251)234-170(284)122(81-111-87-207-95-212-111)227-164(278)114(56-45-71-209-194(205)206)221-168(282)119(77-97(4)5)224-169(283)121(80-110-52-38-35-39-53-110)226-166(280)116(65-68-149(269)270)219-158(272)101(11)213-167(281)118(76-96(2)3)223-163(277)113(55-44-70-208-193(203)204)220-165(279)115(63-66-138(196)257)222-186(300)153(105(15)253)240-159(273)102(12)214-179(293)132-93-308-309-94-133(180(294)231-125(84-141(199)260)174(288)242-152(104(14)252)185(299)215-103(13)160(274)241-154(106(16)254)188(302)237-132)236-162(276)112(54-42-43-69-195)216-145(264)67-64-117(192(306)307)217-144(263)61-40-32-30-28-26-24-22-20-21-23-25-27-29-31-33-41-62-148(267)268/h34-39,50-53,87,95-108,112-137,150-156,249-256H,19-33,40-49,54-86,88-94,195H2,1-18H3,(H2,196,257)(H2,197,258)(H2,198,259)(H2,199,260)(H2,200,261)(H2,201,262)(H2,202,271)(H,207,212)(H,210,297)(H,211,275)(H,213,281)(H,214,293)(H,215,299)(H,216,264)(H,217,263)(H,218,265)(H,219,272)(H,220,279)(H,221,282)(H,222,300)(H,223,277)(H,224,283)(H,225,285)(H,226,280)(H,227,278)(H,228,286)(H,229,291)(H,230,290)(H,231,294)(H,232,301)(H,233,298)(H,234,284)(H,235,292)(H,236,276)(H,237,302)(H,238,287)(H,239,295)(H,240,273)(H,241,274)(H,242,288)(H,243,296)(H,244,289)(H,267,268)(H,269,270)(H,306,307)(H4,203,204,208)(H4,205,206,209)/t100-,101-,102-,103-,104+,105+,106+,107+,108+,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123+,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,150-,151-,152-,153-,154-,155-,156-/m0/s1; Key:LDERDVMBIYGIOI-DDPFBLHVSA-N;

卡格列肽（Cagrilintide）是胰澱粉樣多肽/降鈣素受體雙激動劑，可用來治療肥胖症和II型糖尿病。^[1]^[2]^[3]^[4]^[5]^[6]

研究

卡格列肽（4.5mg）和司美格魯肽結合使用在諾和諾德2期臨床試驗顯示治療肥胖症26周的減重效果達到10.8%。^[7]

參考文獻

^ Larsen, Anna T.; Sonne, Nina; Mohamed, Khaled Elhady; Bredtoft, Emma-Marie; Andersen, Frederik; Karsdal, Morten A.; Henriksen, Kim. 823-P: The Long-Acting Dual Amylin and Calcitonin Receptor Agonist KBP Has Increased Efficacy on Weight Loss and Glucose Control Compared with Cagrilintide in Obese and Diabetic Rats. Diabetes. 1 June 2022, 71 (Supplement_1) [2025-02-08]. S2CID 249259033. doi:10.2337/db22-823-P. （原始內容存檔於2024-04-24）.
^ Lau, David C W; Erichsen, Lars; Francisco, Ann Marie; Satylganova, Altynai; le Roux, Carel W; McGowan, Barbara; Pedersen, Sue D; Pietiläinen, Kirsi H; Rubino, Domenica; Batterham, Rachel L. Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. The Lancet. December 2021, 398 (10317): 2160–2172 [2025-02-08]. PMID 34798060. S2CID 244169045. doi:10.1016/S0140-6736(21)01751-7. （原始內容存檔於2024-12-07）（英語）.
^ Kruse, Thomas; Hansen, Jakob Lerche; Dahl, Kirsten; Schäffer, Lauge; Sensfuss, Ulrich; Poulsen, Christian; Schlein, Morten; Hansen, Ann Maria Kruse; Jeppesen, Claus Bekker; Dornonville de la Cour, Charlotta; Clausen, Trine Ryberg; Johansson, Eva; Fulle, Simone; Skyggebjerg, Rikke Bjerring; Raun, Kirsten. Development of Cagrilintide, a Long-Acting Amylin Analogue. Journal of Medicinal Chemistry. 12 August 2021, 64 (15): 11183–11194. ISSN 0022-2623. PMID 34288673. S2CID 236175929. doi:10.1021/acs.jmedchem.1c00565  （英語）.
^ Frias, Juan P; Deenadayalan, Srikanth; Erichsen, Lars; Knop, Filip K; Lingvay, Ildiko; Macura, Stanislava; Mathieu, Chantal; Pedersen, Sue D; Davies, Melanie. Efficacy and safety of co-administered once-weekly cagrilintide 2·4 mg with once-weekly semaglutide 2·4 mg in type 2 diabetes: a multicentre, randomised, double-blind, active-controlled, phase 2 trial. The Lancet. August 2023, 402 (10403): 720–730. PMID 37364590. S2CID 259237278. doi:10.1016/S0140-6736(23)01163-7 （英語）.
^ D』Ascanio, Antonella M.; Mullally, Jamie A.; Frishman, William H. Cagrilintide: A Long-Acting Amylin Analog for the Treatment of Obesity. Cardiology in Review. 8 March 2023, (Publish Ahead of Print). PMID 36883831. S2CID 257404657. doi:10.1097/CRD.0000000000000513.
^ Larsen, A. T.; Mohamed, K. E.; Sonne, N.; Bredtoft, E.; Andersen, F.; Karsdal, MA; Henriksen, K. Does receptor balance matter? – Comparing the efficacies of the dual amylin and calcitonin receptor agonists cagrilintide and KBP-336 on metabolic parameters in preclinical models. Biomedicine & Pharmacotherapy. 1 December 2022, 156: 113842. ISSN 0753-3322. PMID 36242844. S2CID 252881350. doi:10.1016/j.biopha.2022.113842 .
^ Dutta D, Nagendra L, Harish BG, Sharma M, Joshi A, Hathur B, Kamrul-Hasan A. Efficacy and Safety of Cagrilintide Alone and in Combination with Semaglutide (Cagrisema) as Anti-Obesity Medications: A Systematic Review and Meta-Analysis. Indian Journal of Endocrinology and Metabolism //www.ncbi.nlm.nih.gov/pmc/articles/PMC11642503 |PMC=缺少標題 (幫助). 2024, 28 (5): 436–444. PMC 11642503 . PMID 39676787. doi:10.4103/ijem.ijem_45_24 .

[1] Larsen, Anna T.; Sonne, Nina; Mohamed, Khaled Elhady; Bredtoft, Emma-Marie; Andersen, Frederik; Karsdal, Morten A.; Henriksen, Kim. 823-P: The Long-Acting Dual Amylin and Calcitonin Receptor Agonist KBP Has Increased Efficacy on Weight Loss and Glucose Control Compared with Cagrilintide in Obese and Diabetic Rats. Diabetes. 1 June 2022, 71 (Supplement_1) [2025-02-08]. S2CID 249259033. doi:10.2337/db22-823-P. （原始內容存檔於2024-04-24）.

[2] Lau, David C W; Erichsen, Lars; Francisco, Ann Marie; Satylganova, Altynai; le Roux, Carel W; McGowan, Barbara; Pedersen, Sue D; Pietiläinen, Kirsi H; Rubino, Domenica; Batterham, Rachel L. Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. The Lancet. December 2021, 398 (10317): 2160–2172 [2025-02-08]. PMID 34798060. S2CID 244169045. doi:10.1016/S0140-6736(21)01751-7. （原始內容存檔於2024-12-07）（英語）.

[3] Kruse, Thomas; Hansen, Jakob Lerche; Dahl, Kirsten; Schäffer, Lauge; Sensfuss, Ulrich; Poulsen, Christian; Schlein, Morten; Hansen, Ann Maria Kruse; Jeppesen, Claus Bekker; Dornonville de la Cour, Charlotta; Clausen, Trine Ryberg; Johansson, Eva; Fulle, Simone; Skyggebjerg, Rikke Bjerring; Raun, Kirsten. Development of Cagrilintide, a Long-Acting Amylin Analogue. Journal of Medicinal Chemistry. 12 August 2021, 64 (15): 11183–11194. ISSN 0022-2623. PMID 34288673. S2CID 236175929. doi:10.1021/acs.jmedchem.1c00565  （英語）.

[4] Frias, Juan P; Deenadayalan, Srikanth; Erichsen, Lars; Knop, Filip K; Lingvay, Ildiko; Macura, Stanislava; Mathieu, Chantal; Pedersen, Sue D; Davies, Melanie. Efficacy and safety of co-administered once-weekly cagrilintide 2·4 mg with once-weekly semaglutide 2·4 mg in type 2 diabetes: a multicentre, randomised, double-blind, active-controlled, phase 2 trial. The Lancet. August 2023, 402 (10403): 720–730. PMID 37364590. S2CID 259237278. doi:10.1016/S0140-6736(23)01163-7 （英語）.

[5] D』Ascanio, Antonella M.; Mullally, Jamie A.; Frishman, William H. Cagrilintide: A Long-Acting Amylin Analog for the Treatment of Obesity. Cardiology in Review. 8 March 2023, (Publish Ahead of Print). PMID 36883831. S2CID 257404657. doi:10.1097/CRD.0000000000000513.

[6] Larsen, A. T.; Mohamed, K. E.; Sonne, N.; Bredtoft, E.; Andersen, F.; Karsdal, MA; Henriksen, K. Does receptor balance matter? – Comparing the efficacies of the dual amylin and calcitonin receptor agonists cagrilintide and KBP-336 on metabolic parameters in preclinical models. Biomedicine & Pharmacotherapy. 1 December 2022, 156: 113842. ISSN 0753-3322. PMID 36242844. S2CID 252881350. doi:10.1016/j.biopha.2022.113842 .

[7] Dutta D, Nagendra L, Harish BG, Sharma M, Joshi A, Hathur B, Kamrul-Hasan A. Efficacy and Safety of Cagrilintide Alone and in Combination with Semaglutide (Cagrisema) as Anti-Obesity Medications: A Systematic Review and Meta-Analysis. Indian Journal of Endocrinology and Metabolism //www.ncbi.nlm.nih.gov/pmc/articles/PMC11642503 |PMC=缺少標題 (幫助). 2024, 28 (5): 436–444. PMC 11642503 . PMID 39676787. doi:10.4103/ijem.ijem_45_24 .

[1]

[2]

[3]

[4]

[5]

[6]

[7]