Which female sex hormone, is Deslorelin acetate known to taper off?
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Deslorelin Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. Via its indirect action, following an initial surge the production of sex hormones (Androgen and Estrogen) tapers off.
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Estrogen Estrogen (American English) or oestrogen (British English) is the primary female sex hormone as well as a medication. It is responsible for the development and regulation of the female reproductive system and secondary sex characteristics. "Estrogen" may also refer to any substance, natural or synthetic, that mimics the effects of the natural hormone. The estrane steroid estradiol is the most potent and prevalent endogenous estrogen, although several metabolites of estradiol also have estrogenic hormonal activity. Estrogens are used as medications as part of some oral contraceptives, in hormone replacement therapy for postmenopausal, hypogonadal, and transgender women, and in the treatment of certain hormone-sensitive cancers like prostate cancer and breast cancer. They are one of three types of sex hormones, the others being androgens/anabolic steroids like testosterone and progestogens like progesterone.
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11β-Hydroxyprogesterone 11β-Hydroxyprogesterone (11β-OHP), also known as 21-deoxycorticosterone, as well as 11β-hydroxypregn-4-ene-3,20-dione, is a naturally occurring, endogenous steroid and derivative of progesterone. It is a potent mineralocorticoid. Increased levels of 11β-OHP occur in 21-hydroxylase deficiency.
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Fispemifene Fispemifene (INN, USAN) (developmental code name HM-101) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed for the treatment of male hypogonadism but was abandoned and never marketed. It reached phase II clinical trials for this indication before development was terminated in March 2016. The drug failed to achieve statistical significance on key effectiveness endpoints in clinical trials and was discontinued by its developer for strategic reasons.
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Butagest Butagest, also known as buterol, as well as 3β-hydroxy-6-methyl-17α-hydroxypregna-4,6-dien-20-one 3β-butanoate 17α-acetate or as 6-methyl-17α-hydroxy-δ-progesterone 3β-butanoate 17α-acetate, is a steroidal progestin that was developed in Russia for potential clinical use but was never marketed. It is a modification of megestrol acetate in which the C3 ketone has been replaced with a C3β butanoyloxy moiety.
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Estradiol/progesterone Estradiol/progesterone (developmental code name TX-001HR, formerly TX-12-001HR) is an oral combination of estradiol, an estrogen, and progesterone, a progestogen, that is under development by TherapeuticsMD for the treatment of menopausal symptoms and endometrial hyperplasia. It is currently in phase III clinical trials for these indications. The drug is the first combination of estradiol and progesterone that has been developed for clinical use.
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Flugestone Flugestone (INN, BAN), also known as flurogestone, as well as 9α-fluoro-11β,17α-dihydroxyprogesterone, is a steroidal progestin of the 17α-hydroxyprogesterone group that was never marketed. An acetate ester, flurogestone acetate, is used in veterinary medicine.
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Cetrorelix Cetrorelix (INN, BAN), or cetrorelix acetate (USAN, JAN), is an injectable gonadotropin-releasing hormone (GnRH) antagonist that is marketed primarily under the brand name Cetrotide. A synthetic decapeptide, it is used is used in assisted reproduction to inhibit premature luteinizing hormone surges The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In addition, cetrorelix can be used to treat hormone-sensitive cancers of the prostate and breast (in pre-/perimenopausal women) and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). It is administered as either multiple 0.25 mg daily subcutaneous injections or as a single-dose 3 mg subcutaneous injection. The duration of the 3 mg single dose is four days; if hCG is not administered within four days, a daily 0.25 mg dose is started and continued until hCG is administered.
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Estradiol decanoate Estradiol decanoate (E2D), or estradiol decylate, also known as estradiol 17β-decanoate or as estra-1,3,5(10)-triene-3,17β-diol 17β-decanoate, is a synthetic, steroidal estrogen and an estrogen ester – specifically, the 17β-decanoate (decylate) ester of estradiol – which has been studied for use in hormone replacement therapy for ovariectomized women but was never marketed.
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Ethyldienolone Ethyldienolone, also known as 17α-methyl-19-nor-δ-testosterone, as well as 17α-methylestra-4,9-dien-17β-ol-3-one, is synthetic, orally active anabolic-androgenic steroid (AAS) and a 17α-alkylated derivative of 19-nortestosterone. It is slightly more active than methyltestosterone when given orally. Ethyldienolone is closely related to dienolone and methyldienolone.
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8,9-Dehydroestradiol 8,9-Dehydroestradiol, or Δ-estradiol, also known as estra-1,3,5(10),8-tetraen-17β-ol-3-one, is a naturally occurring steroidal estrogen found in horses that is closely related to equilin, equilenin, and estradiol, and, as the 3-sulfate ester sodium salt, is a minor constituent of conjugated equine estrogens (Premarin). It is also an important active metabolite of 8,9-dehydroestrone, analogously to conversion of estrone or estrone sulfate into estradiol.
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Difelikefalin Difelikefalin (INN) (developmental code names CR845, FE-202845), also known as -Phe--Phe--Leu--Lys-[γ-(4-N-piperidinyl)amino carboxylic acid] (as the acetate salt), is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR). It is under development by Cara Therapeutics as an intravenous agent for the treatment of postoperative pain. An oral formulation has also been developed. Due to its peripheral selectivity, difelikefalin lacks the central side effects like sedation, dysphoria, and hallucinations of previous KOR-acting analgesics such as pentazocine and phenazocine. In addition to use as an analgesic, difelikefalin is also being investigated for the treatment of pruritus (itching). Difelikefalin has completed phase II clinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well-tolerated. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.
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Late-onset hypogonadism Late-onset hypogonadism is a rare condition in older men, characterized by measurably low testosterone levels and clinical symptoms mostly of a sexual nature, including decreased desire for sex, fewer spontaneous erections, and erectile dysfunction. It is the result of a gradual drop in testosterone; a steady decline in testosterone levels of about 1% per year can happen and is well documented in both men and women.
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11-Dehydrocorticosterone 11-Dehydrocorticosterone (11-DHC), also known as 11-oxocorticosterone or 17-deoxycortisone, as well as 21-hydroxypregn-4-ene-3,11,20-trione, is a naturally occurring, endogenous corticosteroid related to cortisone and corticosterone. It is a potent mineralocorticoid, with generally greater such activity than that of corticosterone.
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Anamorelin Anamorelin (INN) (developmental code names ONO-7643, RC-1291, ST-1291), also known as anamorelin hydrochloride (USAN, JAN), is a non-peptide, orally-active, centrally-penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) with appetite-enhancing and anabolic effects which is under development by Helsinn Healthcare SA for the treatment of cancer cachexia and anorexia.
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16α-Hydroxyestrone 16α-Hydroxyestrone (16α-OH-E1), or hydroxyestrone, also known as estra-1,3,5(10)-trien-3,16α-diol-17-one, is an endogenous steroidal estrogen and a major metabolite of estrone, as well as an intermediate in the biosynthesis of estriol. It is a potent estrogen similarly to estrone, and it has been suggested that the ratio of 16α-hydroxyestrone to 2-hydroxyestrone, the latter being much less estrogenic in comparison and even antiestrogenic in the presence of more potent estrogens like estradiol, may be involved in the pathophysiology of breast cancer. Conversely, 16α-hydroxyestrone may help to protect against osteoporosis. In contrast to estradiol, the binding of 16α-hydroxyestrone to the estrogen receptor is, uniquely, covalent and irreversible, and genotoxicity and aberrant hyperproliferations may result. A diacetate ester of 16α-hydroxyestrone, hydroxyestrone diacetate, has been marketed and is used medically as an estrogen in Europe.
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GHRP-6 Growth hormone-releasing peptide 6 (GHRP-6) (developmental code name SKF-110679), also known as growth hormone-releasing hexapeptide, is one of several synthetic met-enkephalin analogues that include unnatural -amino acids, were developed for their growth hormone-releasing activity and are called growth hormone secretagogues. They lack opioid activity but are potent stimulators of growth hormone (GH) release. These secretagogues are distinct from growth hormone releasing hormone (GHRH) in that they share no sequence relation and derive their function through activation of a completely different receptor. This receptor was originally called the growth hormone secretagogue receptor (GHSR), but due to subsequent discoveries, the hormone ghrelin is now considered the receptor's natural endogenous ligand, and it has been renamed as the ghrelin receptor. Therefore, these GHSR agonists act as synthetic ghrelin mimetics.
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17α-Epiestriol 17α-Epiestriol, or simply 17-epiestriol, also known as 16α-hydroxy-17α-estradiol or estra-1,3,5(10)-triene-3,16α,17α-triol, is a minor and weak endogenous estrogen, and the 17α-epimer of estriol (which is 16α-hydroxy-17β-estradiol). It is formed from 16α-hydroxyestrone. In contrast to other endogenous estrogens like estradiol, 17α-epiestriol is a selective agonist of the ERβ. It is described as a relatively weak estrogen, which is in accordance with its relatively low affinity for the ERα. 17α-Epiestriol has been found to be approximately 400-fold more potent than estradiol in inhibiting tumor necrosis factor α (TNFα)-induced vascular cell adhesion molecule 1 (VCAM-1) expression "in vitro".
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Lipoidal estradiol Lipoidal estradiol (LE2) is a collective term that refers to a variety of endogenous C17β long-chain fatty acid esters of estradiol which are formed as metabolites of estradiol. Important examples of these esters include estradiol arachidonate, estradiol lineolate, estradiol oleate, estradiol palmitate, and estradiol stearate. LE2 are estrogens but do not bind to the estrogen receptor, instead acting as prohormones of estradiol. Relative to estradiol, they have far longer-lasting durations of effect due to their much slower rates of metabolism and clearance. It has been hypothesized that LE2 may serve as a store of estrogen for when estradiol levels become low. LE2 are highly lipophilic and hydrophobic and are found in highest concentrations in adipose tissue and other estrogen-sensitive tissues and in low but detectable concentrations in circulation, with none excreted in urine. They have been referred to as the "endogenous counterparts of the synthetic esters of estrogens" like estradiol valerate and estradiol cypionate.
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Premenstrual water retention Premenstrual water retention (or premenstrual fluid retention) is a common phenomenon associated with the menstrual cycle. It consists of the retention of water during the period of time immediately preceding the menstrual cycle (that is, the latter half of the luteal phase, or the week before menstruation). This water retention is most noticeable for its temporary enlargement of the breasts. The excess fluid is lost during menstruation. During this event, the water retention can store enough extra fluid to add an extra 5 – of weight. The phenomenon is thought to be caused by high levels of circulating progesterone, as well as of estrogen and prolactin, stimulating secretory cells in the body and in the breasts. In the breasts, increased blood flow is also thought to be involved. Water retention and breast swelling can also be caused by hormonal contraceptives (which contain estrogen and/or a progestogen).
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11-Deoxycorticosterone 11-Deoxycorticosterone (DOC), or simply deoxycorticosterone, also known as 21-hydroxyprogesterone, as well as desoxycortone (INN), deoxycortone, and cortexone, is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as a precursor to aldosterone. It is an active (Na+-retaining) mineralocorticoid. As its names indicate, 11-deoxycorticosterone can be understood as the 21-hydroxy- variant of progesterone or as the 11-deoxy- variant of corticosterone.
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Follicle-stimulating hormone insensitivity Follicle-stimulating hormone (FSH) insensitivity, or ovarian insensitivity to FSH in females, also referable to as ovarian follicle hypoplasia or granulosa cell hypoplasia in females, is a rare autosomal recessive genetic and endocrine syndrome affecting both females and males, with the former presenting with much greater severity of symptomatology. It is characterized by a resistance or complete insensitivity to the effects of follicle-stimulating hormone (FSH), a gonadotropin which is normally responsible for the stimulation of estrogen production by the ovaries in females and maintenance of fertility in both sexes. The condition manifests itself as hypergonadotropic hypogonadism (decreased or lack of production of sex steroids by the gonads despite high circulating levels of gonadotropins), reduced or absent puberty (lack of development of secondary sexual characteristics, resulting in sexual infantilism if left untreated), amenorrhea (lack of menstruation), and infertility in females, whereas males present merely with varying degrees of infertility and associated symptoms (e.g., decreased sperm production).