Leuprorelin
Clinical data | |
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Trade names | Lupron, Eligard, Lucrin, Lupaneta, others |
Other names | leuprolide, leuprolidine, A-43818, Abbott-43818, DC-2-269, TAP-144 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a685040 |
License data |
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Pregnancy category |
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GnRH agonist; Antigonadotropin | |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Elimination half-life | 3 hours |
Excretion | Kidney |
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Leuprorelin, also known as leuprolide, is a manufactured version of a
Leuprorelin is in the
Leuprorelin was patented in 1973 and approved for medical use in the United States in 1985.[10][12] It is on the World Health Organization's List of Essential Medicines.[11] It is sold under the brand name Lupron among others.[10]
Medical use
Leuprorelin may be used in the treatment of hormone-responsive
It may be used for precocious puberty in both males and females,[14] and to prevent premature ovulation in cycles of controlled ovarian stimulation for in vitro fertilization (IVF). This use is controversial since the Lupron label advises against using the drug when one is considering pregnancy, due to a risk of birth defects.[15]
It may be used to reduce the risk of
Along with
They are also sometimes used as alternatives to antiandrogens like spironolactone and cyproterone acetate for suppressing testosterone production in transgender women.[19][20][21] It also is used for suppressing estrogen production in transgender men.[22]
It is considered a possible treatment for paraphilias.[23] Leuprorelin has been tested as a treatment for reducing sexual urges in pedophiles and other cases of paraphilia.[24][25]
Side effects
Common side effects of leuprorelin injection include redness/burning/stinging/pain/bruising at the injection site, hot flashes (flushing), increased sweating, night sweats, tiredness, headache, upset stomach, nausea, diarrhea, impotence, testicular shrinkage,[8] constipation, stomach pain, breast swelling or tenderness, acne, joint/muscle aches or pain, trouble sleeping (insomnia), reduced sexual interest, vaginal discomfort/dryness/itching/discharge, vaginal bleeding, swelling of the ankles/feet, increased urination at night, dizziness, breakthrough bleeding in a female child during the first two months of leuprorelin treatment, weakness, chills, clammy skin, skin redness, itching, or scaling, testicle pain, impotence, depression, or memory problems.[26] The rates of gynecomastia with leuprorelin have been found to range from 3 to 16%.[27]
A cohort of women that were prescribed leuprorelin to delay precocious puberty as children has developed osteoporosis and brittle teeth at an unexpected rate; However, the FDA has not established that these conditions were caused by leuprorelin.[28]
Pharmacology
Mechanism of action
Leuprorelin is a
Available forms
Leuprorelin is available in the following forms, among others:[31][32][33][34][35]
- Short-acting daily intramuscular injection (Lupron)[4]
- Long-acting depot intramuscular injection (Lupron Depot)[8][36][37][38]
- Long-acting depot subcutaneous injection (Eligard)[5]
- Long-acting subcutaneous injection (Fensolvi)[6]
- Long-acting subcutaneous implant (Viadur)[7]
- Long-acting leuprolide mesylate (Camcevi) for the treatment of advanced prostate cancer.[39]
- Leuprolide acetate and norethindrone acetate co-packaged pack (Lupaneta Pack)[40][41]
Chemistry
The
History
Leuprorelin was discovered and first patented in 1973 and was introduced for medical use in 1985.[42][43] It was initially marketed only for daily injection, but a depot injection formulation was introduced in 1989.[43]
Approvals
- Lupron injection was approved by the FDA for treatment of advanced prostate cancer on 9 April 1985.[44][4][42][43]
- Lupron depot for monthly intramuscular injection was approved by the FDA for palliative treatment of advanced prostate cancer on 26 January 1989.[8]
- Viadur was approved by the FDA for palliative treatment of advanced prostate cancer on 6 March 2000.[7]
- Eligard was approved by the FDA for palliative treatment of advanced prostate cancer on 24 January 2002.[5]
- Fensolvi was approved by the FDA for children with central precocious puberty on 4 May 2020.[6][45]
Society and culture
Legal status
On 24 March 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Camcevi, intended for the treatment of the cancer of the prostate in adult men when the cancer is "hormone-dependent", which means that it responds to treatments that reduce the levels of the hormone testosterone.[46] The applicant for this medicinal product is Accord Healthcare S.L.U.[46] Leuprorelin was approved for medical use in the European Union in May 2022.[9][47]
Names
Leuprorelin is the
Leuprorelin is marketed by Bayer AG under the brand name Viadur,[7] by Tolmar under the brand names Eligard and Fensolvi,[5][6] and by TAP Pharmaceuticals (1985–2008), by Varian Darou Pajooh under the brand name Leupromer and Abbott Laboratories (2008–present) under the brand name Lupron.
Controversy
In October 2001, the US Department of Justice, states attorneys general, and TAP Pharmaceutical Products, a subsidiary of Abbott Laboratories, settled criminal and civil charges against TAP related to federal and state
There have since been various suits concerning leuprorelin use, none successful.[55][56] They either concern the oversubscription of the drug or undue warning about the side effects. Between 2010 and 2013, the FDA updated the Lupron drug label to include new safety information on the risk of thromboembolism, loss of bone density and convulsions.[57] The FDA then asserted that the benefits of leuprorelin outweigh its risks when used according to its approved labeling. Since 2017, the FDA has been evaluating leuprorelin's connection to pain and discomfort in musculoskeletal and connective tissue.[58]
Research
As of 2006[update], leuprorelin was under investigation for possible use in the treatment of mild to moderate Alzheimer's disease.[59][needs update]
A
Veterinary use
Leuprorelin is frequently used in ferrets for the treatment of
References
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- ^ a b c d "Eligard- leuprolide acetate kit". DailyMed. 26 March 2020. Archived from the original on 10 August 2020. Retrieved 20 August 2020.
- ^ a b c d "Fensolvi- leuprolide acetate kit". DailyMed. 3 June 2020. Archived from the original on 26 October 2020. Retrieved 20 August 2020.
- ^ a b c d "Viadur- leuprolide acetate". DailyMed. Archived from the original on 27 May 2021. Retrieved 26 May 2021.
- ^ a b c d "Lupron Depot- leuprolide acetate kit". DailyMed. Archived from the original on 27 May 2021. Retrieved 27 May 2021.
- ^ a b "Camcevi EPAR". European Medicines Agency (EMA). 22 March 2022. Retrieved 21 June 2022.
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Table 1
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- ^ "Lupaneta Pack- leuprolide acetate and norethindrone acetate kit". DailyMed. Archived from the original on 27 May 2021. Retrieved 27 May 2021.
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Further reading
- Shajnfeld A, Krueger RB (July 2006). "Reforming (Purportedly) Non-Punitive Responses to Sexual Offending". Developments in Mental Health Law. 25: 81. SSRN 1077282.