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User:Mr. Ibrahem/Histrelin

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Mr. Ibrahem/Histrelin
Clinical data
Trade namesVantas, Supprelin LA, others
Other namesHistrelin acetate
AHFS/Drugs.comMonograph
MedlinePlusa601146
Routes of
administration		Subcutaneous implant
Drug classGnRH agonist; Antigonadotropin
Legal status
Legal status
Pharmacokinetic data
Bioavailability92%
Protein binding70%
MetabolismLiver
Elimination half-life4.0 hours
Identifiers
  • 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-N5-(diaminomethylene)-L-ornithyl-N-ethyl-L-prolinamide
Chemical and physical data
FormulaC66H86N18O12
Molar mass1323.528 g·mol−1
3D model (JSmol)
  • CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CN(C=N2)CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CNC=N7)NC(=O)[C@@H]8CCC(=O)N8
  • InChI=1S/C66H86N18O12/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71)/t47-,48-,49-,50-,51-,52-,53+,54-,55-/m0/s1 checkY
  • Key:HHXHVIJIIXKSOE-QILQGKCVSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Histrelin, sold under the brand names Vantas among others, is a medication used to treat advanced prostate cancer.[1] It may also be used for precocious puberty and in transgender children.[2][3] It is given by injection under the skin.[1]

Common side effects include pain at the site of injection, hot flashes, breast enlargement, sexual dysfunction, tiredness, kidney problems, constipation, weight loss, and trouble sleeping.[1] Other side effects may include osteoporosis, high blood sugar, liver problems, anaphylaxis, and pituitary apoplexy.[1] Use in pregnancy may harm the baby.[1] It acts similar to gonadotropin-releasing hormone (GnRH), resulting in increased luteinizing hormone (LH) and follicle stimulating hormone (FSH), and therefore decreased testosterone and estrogen.[1][3]

Histrelin was approved for medical use in the United States in 1991.[1] It is available as a generic medication.[3] In the United States an implant costs about 5,100 USD per year as of 2021.[4] Since 2014 it is no longer commercially available in the United Kingdom.[5]

References[edit]

  1. ^ a b c d e f g h i "Histrelin Monograph for Professionals". Drugs.com. Archived from the original on 29 August 2019. Retrieved 10 December 2021.
  2. ^ "Primary Care Protocol for Transgender Patient Care: Hormone Administration". transhealth.ucsf.edu. Archived from the original on 2012-01-17. Retrieved 2015-09-29.
  3. ^ a b c "Histrelin". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 11 December 2021. Retrieved 10 December 2021.
  4. ^ "Vantas Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 22 July 2021. Retrieved 10 December 2021.
  5. ^ "Vantas (discontinued in the UK - September 2014)". Netdoctor. 28 September 2012. Archived from the original on 4 November 2021. Retrieved 10 December 2021.
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