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EPI-001
EPI-001 is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of EPI-001, EPI-002, is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.). EPI-001 and its stereoisomers and analogues were discovered by Marianne Sadar and Raymond Andersen, who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC). EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice varian ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ralaniten Acetate
Ralaniten acetate (developmental code name EPI-506) is a first-in-class antiandrogen that targets the ''N''-terminal domain (NTD) of the androgen receptor (AR) developed by ESSA Pharmaceuticals and was under investigation for the treatment of prostate cancer. This mechanism of action is believed to allow the drug to block signaling from the AR and its splice variants. EPI-506 is a derivative of bisphenol A and a prodrug of ralaniten (EPI-002), one of the four stereoisomers of EPI-001, and was developed as a successor of EPI-001. The drug reached phase I/ II prior to the discontinuation of its development. It showed signs of efficacy in the form of prostatic specific antigen (PSA) decreases (4–29%) predominantly at higher doses (≥1,280 mg) in some patients but also caused side effects and was discontinued by its developer in favor of next-generation AR NTD inhibitors with improved potency and tolerability. See also * EPI-7386 EPI-7386 is an ''N''-terminal doma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ralaniten
Ralaniten (developmental code name EPI-002) is an N-terminal domain antiandrogen which was never marketed. It is a derivative (chemistry), derivative of bisphenol A and one of the four stereoisomers of EPI-001. A prodrug of ralaniten, ralaniten acetate (EPI-506), was under development for the treatment of prostate cancer. See also * EPI-7386 References Abandoned drugs Alkylating agents 2,2-Bis(4-hydroxyphenyl)propanes Halohydrins Nonsteroidal antiandrogens Organochlorides Polyols Glycerols {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen Receptor
The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression; however, the androgen receptor has other functions as well. Androgen-regulated genes are critical for the development and maintenance of the male sexual phenotype. Function Effect on development In some cell types, testosterone interacts directly with androgen receptors, whereas, in others, testosterone is converted by 5-alpha-reductase to dihydrotestosterone, an even more potent agonist for androgen receptor activation. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EPI-7386
EPI-7386 is an N-terminal domain antiandrogen, ''N''-terminal domain antiandrogen, or receptor antagonist, antagonist of the N-terminal domain, ''N''-terminal domain (NTD) of the androgen receptor (AR), which is under development for the treatment of prostate cancer. The compound was developed as a successor of previous drugs in the EPI series such as EPI-001, ralaniten (EPI-002), and ralaniten acetate (EPI-506). EPI-7386 shows 20-fold higher antiandrogenic potency (pharmacology), potency than ralaniten ''in vitro'' ( = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes. It is planned to enter Phases of clinical research#Phase I, phase I clinical trials in 2020. References Experimental cancer drugs Nonsteroidal antiandrogens {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EPI-002
Ralaniten (developmental code name EPI-002) is an N-terminal domain antiandrogen which was never marketed. It is a derivative of bisphenol A and one of the four stereoisomers of EPI-001. A prodrug of ralaniten, ralaniten acetate (EPI-506), was under development for the treatment of prostate cancer. See also * EPI-7386 EPI-7386 is an N-terminal domain antiandrogen, ''N''-terminal domain antiandrogen, or receptor antagonist, antagonist of the N-terminal domain, ''N''-terminal domain (NTD) of the androgen receptor (AR), which is under development for the treatment ... References Abandoned drugs Alkylating agents 2,2-Bis(4-hydroxyphenyl)propanes Halohydrins Nonsteroidal antiandrogens Organochlorides Polyols Glycerols {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective PPARγ Modulator
A selective PPAR modulator (SPPARM) is a selective receptor modulator of the peroxisome proliferator-activated receptor (PPAR). Examples include SPPARMs of the PPARγ, BADGE, EPI-001, INT-131, MK-0533, and S26948. See also * PPAR agonist PPAR agonists are drugs which act upon the peroxisome proliferator-activated receptor. They are used for the treatment of symptoms of the metabolic syndrome, mainly for lowering triglycerides and blood sugar. Classification PPAR-alpha and PPAR-g ... References PPAR agonists {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CREB-binding Protein
Cyclic adenosine monophosphate Response Element Binding protein Binding Protein (CREB-binding protein), also known as CREBBP or CBP or KAT3A, is a coactivator encoded by the ''CREBBP'' gene in humans, located on chromosome 16p13.3. CBP has intrinsic acetyltransferase functions; it is able to add acetyl groups to both transcription factors as well as histone lysines, the latter of which has been shown to alter chromatin structure making genes more accessible for transcription. This relatively unique acetyltransferase activity is also seen in another transcription enzyme, EP300 (p300). Together, they are known as the p300-CBP coactivator family and are known to associate with more than 16,000 genes in humans; however, while these proteins share many structural features, emerging evidence suggests that these two co-activators may promote transcription of genes with different biological functions. For example, CBP alone has been implicated in a wide variety of pathophysiologies inclu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonsteroidal Antiandrogens
A nonsteroidal antiandrogen (NSAA) is an antiandrogen with a nonsteroidal chemical structure. They are typically binding selectivity, selective and silent antagonist, full or silent antagonists of the androgen receptor (AR) and act by directly receptor antagonist, blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). NSAAs are used in the treatment of androgen-dependent conditions in men and women. They are the converse of steroidal antiandrogens (SAAs), which are antiandrogens that are steroids and are structurally related to testosterone. Medical uses NSAAs are used in clinical medicine for the following indications: * Prostate cancer in men * Androgen-dependent condition, Androgen-dependent dermatological condition, skin and hair conditions like acne, hirsutism, seborrhea, and pattern hair loss (androgenic alopecia) in women * Hyperandrogenism, such as due to polycystic ovary syndrome or congenital adrenal hyperplasia, in women * As a component of ho ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,2-Bis(4-hydroxyphenyl)propanes
The comma is a punctuation mark that appears in several variants in different languages. It has the same shape as an apostrophe or single closing quotation mark () in many typefaces, but it differs from them in being placed on the baseline of the text. Some typefaces render it as a small line, slightly curved or straight, but inclined from the vertical. Other fonts give it the appearance of a miniature filled-in figure on the baseline. The comma is used in many contexts and languages, mainly to separate parts of a sentence such as clauses, and items in lists mainly when there are three or more items listed. The word ''comma'' comes from the Greek (), which originally meant a cut-off piece, specifically in grammar, a short clause. A comma-shaped mark is used as a diacritic in several writing systems and is considered distinct from the cedilla. In Byzantine and modern copies of Ancient Greek, the " rough" and "smooth breathings" () appear above the letter. In Latvi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkylating Agents
Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effecting alkylation. Alkyl groups can also be removed in a process known as dealkylation. Alkylating agents are often classified according to their nucleophilic or electrophilic character. In oil refining contexts, alkylation refers to a particular alkylation of isobutane with olefins. For upgrading of petroleum, alkylation produces a premium blending stock for gasoline. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Nucleophilic alkylating agents Nucleophilic alkylating agents deliver the equivalent of an alkyl anion (carbanion). The formal "alkyl anion" attacks an electrophile, forming a new covalent bond be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aban ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
