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Androgen Receptor Degrader
A (selective) androgen receptor degrader or downregulator (SARD) is a type of drug which interacts with the androgen receptor (AR) such that it causes the AR to be degraded and thus downregulated. They are under investigation for the treatment of prostate cancer and other androgen-dependent conditions. As of 2017, dimethylcurcumin (ASC-J9), a SARD, is under development for the treatment of acne vulgaris. In addition, several PROTACs degraders targeting the androgen receptor have been tested in the clinic: # Bavdegalutamide (ARV-110): Developed by Arvinas, this PROTAC is currently in phase 2 clinical trials and has shown encouraging results for patients with metastatic castration-resistant prostate cancer. # Luxdegalutamide (ARV-766) Developed by Arvinas, this second-generation AR PROTAC has advanced to phase II clinical trials. It was designed to overcome some limitations of ARV-110, particularly in targeting the AR L702H mutation. # Gridegalutamide (CC-94676, AR-LDD): Init ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmaceutical Drug
Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and relies on the science of pharmacology for continual advancement and on pharmacy for appropriate management. Drugs are classified in many ways. One of the key divisions is by level of control, which distinguishes prescription drugs (those that a pharmacist dispenses only on the medical prescription) from over-the-counter drugs (those that consumers can order for themselves). Medicines may be classified by mode of action, route of administration, biological system affected, or therapeutic effects. The World Health Organization keeps a list of essential medicines. Drug discovery and drug development are complex and expensive endeavors undertaken by pharmaceutical companies, academic scientists, and governments. As ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiandrogens
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production. They can be thought of as the functional opposites of AR agonists, for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiprogestogens. Antiandrogens are used to treat an assortment of androgen-dependent conditions. In men, antiandrogens are used in the treatment of prostate cancer, enlarged prostate, scalp hair loss, overly high sex drive, unusual and problematic sexual urges, and early puberty. In women, antiandrogens are used to treat acne, sebo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androgen Deprivation Therapy
Androgen deprivation therapy (ADT), also called androgen ablation therapy or androgen suppression therapy, is an antihormone therapy whose main use is in treating prostate cancer. Prostate cancer cells usually require androgen, androgen hormones, such as testosterone, to grow. ADT reduces the levels of androgen hormones, with pharmaceutical drug, drugs or surgery, to prevent the prostate cancer cells from growing. The pharmaceutical approaches include antiandrogens and chemical castration. Several studies have concluded that ADT has demonstrated benefit in patients with metastatic disease, and as an adjunct to radiation therapy in patients with locally advanced disease, as well as those with unfavorable intermediate-risk or high-risk localized disease. However, in patients with low-risk prostate cancer, ADT has demonstrated no survival advantage, and significant harm, such as impotence, diabetes and bone loss. The therapy can also eliminate cancer cells by inducing androgen depriv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bristol Myers Squibb
The Bristol-Myers Squibb Company, Trade name, doing business as Bristol Myers Squibb (BMS), is an American multinational pharmaceutical company. Headquartered in Princeton, New Jersey, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the Fortune 500, ''Fortune'' 500 list of the largest U.S. corporations. For fiscal year, fiscal 2022, it had a total revenue of $46.2 billion. Bristol Myers Squibb manufactures prescription pharmaceuticals and Biopharmaceutical, biologics in several therapeutic areas, including cancer, HIV/AIDS, cardiovascular disease, diabetes, hepatitis, rheumatoid arthritis, and psychiatric disorders. BMS's primary research and development (R&D) sites are located in Lawrence Township, Mercer County, New Jersey, Lawrence, New Jersey (formerly Squibb, near Princeton), Summit, New Jersey, formerly HQ of Celgene, New Brunswick, New Jersey; Redwood City, California; and Seville in Spain, with other sites in Devens, Massachuset ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Celgene
Celgene Corporation, headquartered in Summit, New Jersey, was a pharmaceutical company that produced cancer and immunology drugs. Its primary products were Revlimid (lenalidomide), which is used in the treatment of multiple myeloma (63% of 2018 revenues); Pomalyst and Imnovid (Pomalidomide), also used in the treatment of multiple myeloma (13% of 2018 revenues); and Otezla (Apremilast), used in the treatment of psoriasis (11% of 2018 revenues). In 2018, 66% of the company's revenues came from the United States. In 2019, the company was acquired by Bristol Myers Squibb (BMS); as part of the acquisition, Otezla was sold to Amgen. History Celgene was originally a unit of Celanese. In 1986, Celanese completed the corporate spin-off of Celgene following the merger of Celanese with Hoechst AG, American Hoechst. In August 2000, Celgene acquired Signal Pharmaceuticals, Inc., a privately held company that developed pharmaceuticals to regulate disease-related genes. Signal Pharmaceuticals w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gridegalutamide
Gridegalutamide is an investigational oral androgen receptor (AR) degrader being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system. CC-94676 employs a unique dual mechanism of action, combining AR degradation with AR antagonism, potentially offering advantages over traditional AR inhibitors in overcoming resistance mechanisms. Initially developed by Celgene and now under Bristol Myers Squibb, CC-94676 has demonstrated AR protein degradation and suppression of tumor growth in CRPC mouse models. As of 2024, CC-94676 is being evaluated in phase I clinical trials for patients with mCRPC who have progressed on androgen deprivation therapy Androgen deprivation therapy (ADT), also called androgen ablation therapy or androgen suppression therapy, is an antihormone t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Luxdegalutamide
Luxdegalutamide, also known as ARV-766 and JSB462, is an investigational oral androgen receptor (AR) degrader being developed by Arvinas for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system. Luxdegalutamide is a second-generation PROTAC AR degrader that has demonstrated a broader efficacy profile and better tolerability compared to its predecessor, ARV-110, in clinical settings. It has shown promise in overcoming resistance associated with certain AR mutations, including the L702H mutation, which is prevalent in up to 24% of treated mCRPC patients. As of 2024, luxdegalutamide is being evaluated in phase I/II clinical trials for prostate cancer. Mechanism of action Luxdegalutamide is a heterobifunctional PROTAC that targets the androgen receptor for degradation. Unlike conve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bavdegalutamide
Bavdegalutamide is an experimental proteolysis targeting chimera that functions as a androgen receptor degrader. It is being developed to treat metastatic castration-resistant prostate cancer Prostate cancer is the neoplasm, uncontrolled growth of cells in the prostate, a gland in the male reproductive system below the bladder. Abnormal growth of the prostate tissue is usually detected through Screening (medicine), screening tests, .... References {{Genito-urinary-drug-stub Receptor degraders Glutarimides Phthalimides Piperazines Piperidines Pyridazines Cyclohexanes Benzonitriles Chlorobenzene derivatives Phenyl compounds ... [...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 Cell nucleus, 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 protein, DNA-binding transcription factor that Gene expression regulation, 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, 5-alpha-reductase to dihydrot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acne Vulgaris
Acne ( ), also known as ''acne vulgaris'', is a long-term Cutaneous condition, skin condition that occurs when Keratinocyte, dead skin cells and Sebum, oil from the skin clog hair follicles. Typical features of the condition include comedo, blackheads or whiteheads, pimples, oily skin, and possible scarring. It primarily affects skin with a relatively high number of sebaceous gland, oil glands, including the face, upper part of the chest, and back. The resulting appearance can lead to lack of confidence, anxiety (mood), anxiety, reduced self-esteem, and, in extreme cases, clinical depression, depression or suicidal ideations, thoughts of suicide. Susceptibility to acne is primarily genetic in 80% of cases. The roles of diet and cigarette smoking in the condition are unclear, and neither hygiene, cleanliness nor exposure to sunlight are associated with acne. In both sexes, hormones called androgens appear to be part of the underlying mechanism, by causing increased production ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
