Teduglutide

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Teduglutide
Names
Trade namesGattex, Revestive, others
  • L-histidylglycyl-L-α-aspartylglycyl-L-seryl-L-phenylalanyl-L-seryl-L-α-aspartyl-L-α-glutamyl-L-methionyl-L-asparaginyl-L-threonyl-L-isoleucyl-L-leucyl-L-α-aspartyl-L-asparaginyl-L-leucyl-L-alanyl-L-alanyl-L-arginyl-L-α-aspartyl-L-phenylalanyl-L-isoleucyl-L-asparaginyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-glutaminyl-L-threonyl-L-lysyl-L-isoleucyl-L-threonyl-L-aspartic acid
Clinical data
Drug classGlucagon-like peptide-2 (GLP-2)[1]
Main usesShort bowel syndrome[1]
Side effectsAbdominal pain, nausea, fluid overload, allergic reactions, headache[1]
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
use		Subcutaneous injection
Typical dose0.05mg/kg OD[1]
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Pharmacokinetics
Bioavailability88%
MetabolismProteolysis
Elimination half-life2 h
Chemical and physical data
FormulaC164H252N44O55S
Molar mass3752.13 g·mol−1
3D model (JSmol)
  • CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O
  • InChI=1S/C164H252N44O55S/c1-21-77(11)126(156(255)187-95(44-46-114(167)214)141(240)206-130(83(17)211)160(259)186-93(42-33-34-49-165)140(239)202-129(80(14)24-4)159(258)208-131(84(18)212)161(260)200-111(163(262)263)66-125(230)231)203-151(250)100(54-76(9)10)189-145(244)103(57-88-67-175-92-41-32-31-40-90(88)92)192-147(246)105(60-116(169)216)199-157(256)127(78(12)22-2)204-152(251)102(56-87-38-29-26-30-39-87)190-149(248)109(64-123(226)227)195-137(236)94(43-35-50-174-164(171)172)183-134(233)82(16)179-133(232)81(15)180-142(241)98(52-74(5)6)188-146(245)104(59-115(168)215)194-150(249)110(65-124(228)229)196-143(242)99(53-75(7)8)198-158(257)128(79(13)23-3)205-162(261)132(85(19)213)207-153(252)106(61-117(170)217)193-139(238)97(48-51-264-20)185-138(237)96(45-47-120(220)221)184-148(247)108(63-122(224)225)197-155(254)113(72-210)201-144(243)101(55-86-36-27-25-28-37-86)191-154(253)112(71-209)182-119(219)70-177-136(235)107(62-121(222)223)181-118(218)69-176-135(234)91(166)58-89-68-173-73-178-89/h25-32,36-41,67-68,73-85,91,93-113,126-132,175,209-213H,21-24,33-35,42-66,69-72,165-166H2,1-20H3,(H2,167,214)(H2,168,215)(H2,169,216)(H2,170,217)(H,173,178)(H,176,234)(H,177,235)(H,179,232)(H,180,241)(H,181,218)(H,182,219)(H,183,233)(H,184,247)(H,185,237)(H,186,259)(H,187,255)(H,188,245)(H,189,244)(H,190,248)(H,191,253)(H,192,246)(H,193,238)(H,194,249)(H,195,236)(H,196,242)(H,197,254)(H,198,257)(H,199,256)(H,200,260)(H,201,243)(H,202,239)(H,203,250)(H,204,251)(H,205,261)(H,206,240)(H,207,252)(H,208,258)(H,220,221)(H,222,223)(H,224,225)(H,226,227)(H,228,229)(H,230,231)(H,262,263)(H4,171,172,174)/t77-,78-,79-,80-,81-,82-,83+,84+,85+,91-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,126-,127-,128-,129-,130-,131-,132-/m0/s1 checkY
  • Key:CILIXQOJUNDIDU-ASQIGDHWSA-N checkY

Teduglutide, sold under the brand names Gattex among others is a medication used for short bowel syndrome.[1] Specifically it is used for people who require parenteral nutrition.[1] It is given by injection just under the skin.[1]

Common side effects include abdominal pain, nausea, fluid overload, allergic reactions, and headache.[1] Other potential side effects may include tumors, intestinal obstruction, gall bladder disease, and pancreatitis.[1] Use during pregnancy appears to be safe.[2] It is similar to the bodies own glucagon-like peptide-2 (GLP-2), which increases the uptake of nutrients from the intestines.[3]

Teduglutide was approved for medical use in the United States and Europe in 2012.[1][3] At a dose of 5 mg per day, in the United Kingdom it costs the NHS about £15,000 a month as of 2021.[4] This amount in the United States costs about 36,000 per month.[5]

Medical uses

Up to a certain point, the gut can adapt to partial resections that result in short bowel syndrome. Still, parenteral substitution of water, minerals and vitamins (depending on which part of the gut has been removed) is often necessary. Teduglutide may reduce or shorten the necessity of such infusions by improving the intestinal mucosa and possibly by other mechanisms.[6]

Dosage

It is generally give at a dose of 0.05 mg per kg once per day.[1] Half that dose may be used in those with moderate to severe kidney dysfunction.[3]

Side effects

Common side effects included abdominal discomfort (49%), respiratory infections (28%), nausea (27%) and vomiting (14%), local reactions at the injection site (21%), and headache (17%).[6]

Mechanism of action

Teduglutide differs from natural GLP-2 by a single amino acid: an alanine is replaced with a glycine. This blocks breaking down of the molecule by dipeptidyl peptidase and increases its half-life from seven minutes (GLP-2) to about two hours, while retaining its biological actions. These include maintenance of the intestinal mucosa, increasing intestinal blood flow, reducing gastrointestinal motility and secretion of gastric acid.[6]

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 "Teduglutide Monograph for Professionals". Drugs.com. Archived from the original on 4 March 2021. Retrieved 24 September 2021.
  2. ↑ "Teduglutide (Gattex) Use During Pregnancy". Drugs.com. Archived from the original on 25 January 2021. Retrieved 24 September 2021.
  3. ↑ 3.0 3.1 3.2 "Revestive". Archived from the original on 12 November 2020. Retrieved 24 September 2021.
  4. ↑ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 54. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  5. ↑ "Specialty drug prices soaring past six figures per year". KSAT. 26 July 2019. Archived from the original on 26 November 2020. Retrieved 24 September 2021.
  6. ↑ 6.0 6.1 6.2 Klement A (5 January 2015). "Das Kurzdarmsyndrom ist erstmals behandelbar: Revestive". Österreichische Apothekerzeitung (in German) (1/2015): 20f.{{cite journal}}: CS1 maint: unrecognized language (link)

External links

Identifiers:
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