LGD-2941

Last updated
LGD-2941
LGD-2941.svg
Identifiers
  • 6-[(2R,5R)-2-methyl-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1H-quinolin-2-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C17H16F6N2O2
Molar mass 394.317 g·mol−1
3D model (JSmol)
  • C[C@@H]1CC[C@@H](N1C2=CC3=C(C=C2)NC(=O)C=C3C(F)(F)F)[C@H](C(F)(F)F)O
  • InChI=InChI=1S/C17H16F6N2O2/c1-8-2-5-13(15(27)17(21,22)23)25(8)9-3-4-12-10(6-9)11(16(18,19)20)7-14(26)24-12/h3-4,6-8,13,15,27H,2,5H2,1H3,(H,24,26)/t8-,13-,15-/m1/s1
  • Key:HWLLYFXDDGGHOE-BCSUUIJWSA-N

LGD-2941 is a drug which acts as a selective androgen receptor modulator (SARM). [1] It is no longer being developed. [2]

Related Research Articles

A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents.

<span class="mw-page-title-main">Selective androgen receptor modulator</span> Class of pharmaceutical drugs

Selective androgen receptor modulators (SARMs) are a class of drugs that selectively activate the androgen receptor in certain tissues like muscle and bone over other tissues like the prostate gland and seminal vesicles.

<span class="mw-page-title-main">BMS-564,929</span> Chemical compound

BMS-564,929 is an investigational selective androgen receptor modulator (SARM) which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men ("andropause"). These symptoms may include depression, loss of muscle mass and strength, reduction in libido and osteoporosis. Treatment with exogenous testosterone is effective in counteracting these symptoms but is associated with a range of side effects, the most serious of which is enlargement of the prostate gland, which can lead to benign prostatic hypertrophy and even prostate cancer. This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in the prostate.

<span class="mw-page-title-main">S-40503</span> Chemical compound

S-40503 is an investigational selective androgen receptor modulator (SARM) developed by the Japanese company Kaken Pharmaceuticals, which was developed for the treatment of osteoporosis. SARMs are a new class of drugs which produce tissue-specific anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in other tissues such as in the prostate gland, thus avoiding side effects such as benign prostatic hypertrophy which can occur following treatment with unselective androgens like testosterone or anabolic steroids.

<span class="mw-page-title-main">LGD-2226</span> Chemical compound

LGD-2226 is an investigational selective androgen receptor modulator (SARM), which is being developed for treatment of muscle wasting and osteoporosis.

<span class="mw-page-title-main">Enobosarm</span> Investigational selective androgen receptor modulator

Enobosarm, also formerly known as ostarine and by the developmental code names GTx-024, MK-2866, and S-22, is a selective androgen receptor modulator (SARM) which is under development for the treatment of androgen receptor-positive breast cancer in women and for improvement of body composition in people taking GLP-1 receptor agonists like semaglutide. It was also under development for a variety of other indications, including treatment of cachexia, Duchenne muscular dystrophy, muscle atrophy or sarcopenia, and stress urinary incontinence, but development for all other uses has been discontinued. Enobosarm was evaluated for the treatment of muscle wasting related to cancer in late-stage clinical trials, and the drug improved lean body mass in these trials, but it was not effective in improving muscle strength. As a result, enobosarm was not approved and development for this use was terminated. Enobosarm is taken by mouth.

<span class="mw-page-title-main">Andarine</span> Chemical compound

Andarine is a selective androgen receptor modulator (SARM) which was developed by GTX, Inc for the treatment of conditions such as muscle wasting, osteoporosis, and benign prostatic hypertrophy (BPH), using the nonsteroidal antiandrogen bicalutamide as a lead compound. Development of andarine for all indications has been discontinued, in favor of the structurally related and improved compound enobosarm.

<span class="mw-page-title-main">AC-262,536</span> Chemical compound

AC-262536 is a drug developed by Acadia Pharmaceuticals which acts as a selective androgen receptor modulator (SARM). Chemically it possesses endo-exo isomerism, with the endo form being the active form. It acts as a partial agonist for the androgen receptor with a Ki of 5 nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of the levator ani muscle weight increase of testosterone, but only around 27% of its maximal effect on prostate gland weight. It is an aniline SARM related to ACP-105 and vosilasarm (RAD140).

<span class="mw-page-title-main">S-23 (drug)</span> Investigational selective androgen receptor modulator

S-23 is an investigational selective androgen receptor modulator (SARM) developed by GTX, Inc as a potential male hormonal contraceptive. It binds to the androgen receptor more strongly than older drugs such as andarine with a Ki of 1.7 nM, and in animal studies it showed both a good ratio of anabolic to androgenic effects, and dose-dependent suppression of spermatogenesis with spontaneous recovery after cessation of treatment.

<span class="mw-page-title-main">LGD-3303</span> Chemical compound

LGD-3303 is a drug which acts as a selective androgen receptor modulator (SARM), with good oral bioavailability. It is a selective agonist for the androgen receptor, producing functional selectivity with effective dissociation of anabolic and androgenic effects, acting as a partial agonist for androgenic effects, but a full agonist for anabolic effects. It has been investigated as a possible treatment for osteoporosis, and was shown in animal studies to enhance the effectiveness of a bisphosphonate drug.

<span class="mw-page-title-main">Ligandrol</span> Chemical compound

Ligandrol, also known by the developmental code names VK5211 and LGD-4033, is a selective androgen receptor modulator (SARM) which is under development for the treatment of muscle atrophy in people with hip fracture. It was also under development for the treatment of cachexia, hypogonadism, and osteoporosis, but development for these indications was discontinued. Ligandrol has been reported to dose-dependently improve lean body mass and muscle strength in preliminary clinical trials, but is still being developed and has not been approved for medical use. The drug is taken by mouth.

<span class="mw-page-title-main">Vosilasarm</span> Chemical compound

Vosilasarm, also known by the development codes RAD140 and EP0062 and by the black-market name Testolone or Testalone, is a selective androgen receptor modulator (SARM) which is under development for the treatment of hormone-sensitive breast cancer. It is specifically under development for the treatment of androgen receptor-positive, estrogen receptor-negative, HER2-negative advanced breast cancer. Vosilasarm was also previously under development for the treatment of sarcopenia, osteoporosis, and weight loss due to cancer cachexia, but development for these indications was discontinued. The drug is taken by mouth.

<span class="mw-page-title-main">LG121071</span> Chemical compound

LG121071 is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered. It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine). The drug acts as a high-affinity full agonist of the androgen receptor (AR), with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT). Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues, and for this reason, show tissue-selective androgenic effects. In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids.

A sex-hormonal agent, also known as a sex-hormone receptor modulator, is a type of hormonal agent which specifically modulates the effects of sex hormones and of their biological targets, the sex hormone receptors. The sex hormones include androgens such as testosterone, estrogens such as estradiol, and progestogens such as progesterone. Sex-hormonal agents may be either steroidal or nonsteroidal in chemical structure and may serve to either enhance, inhibit, or have mixed effects on the function of the sex hormone systems.

<span class="mw-page-title-main">EM-5854</span> Chemical compound

EM-5854 is a steroidal antiandrogen which was under development by Endoceutics, Inc. for the treatment of prostate cancer. It was first described in a patent in 2008, and was further characterized in 2012. EM-5854 reached phase I/II clinical trials for the treatment of prostate cancer but development was discontinued in March 2019.

<span class="mw-page-title-main">OPK-88004</span> Chemical compound

OPK-88004 is a non-steroidal indole derivative which acts as a selective androgen receptor modulator (SARM). It has been investigated by OPKO Health for the treatment of erectile dysfunction and symptoms associated with benign prostate hyperplasia.

<span class="mw-page-title-main">GLPG-0492</span> Medication

GLPG-0492 (DT-200) is a drug which acts as a selective androgen receptor modulator (SARM). It has been investigated for the treatment of cachexia and muscular dystrophy.

<span class="mw-page-title-main">ACP-105</span> Chemical compound

ACP-105 is a drug which acts as a selective androgen receptor modulator (SARM). It has been investigated for potential use in the treatment of age-related cognitive decline. The drug has been found to reduce anxiety-like behavior in a mouse model of Alzheimer's disease when administered alone, as well as enhance spatial memory when coadministered with the selective estrogen receptor β agonist AC-186. ACP-105 is an aniline SARM and is related to AC-262536 and vosilasarm (RAD140).

<span class="mw-page-title-main">GSK-4336A</span> Chemical compound

GSK4336A is a drug which acts as a selective androgen receptor modulator (SARM), and was developed for androgen replacement therapy.

References

  1. ↑ Long YO, Higuchi RI, Caferro TR, Lau TL, Wu M, Cummings ML, Martinborough EA, Marschke KB, Chang WY, López FJ, Karanewsky DS, Zhi L (May 2008). "Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity". Bioorganic & Medicinal Chemistry Letters. 18 (9): 2967–71. doi:10.1016/j.bmcl.2008.03.062. PMID   18400499.
  2. ↑ "LGD 2941". AdisInsight. Springer Nature Switzerland AG.
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