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Restrict the search for
phenylacetate
to a specific field?
Status:
US Approved Rx
(2009)
Source:
ANDA040844
(2009)
Source URL:
First approved in 1961
Source:
NDA012827
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Glycopyrrolate is a synthetic anticholinergic agent with a quaternary ammonium structure. Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. Glycopyrrolate binds competitively to the muscarinic acetylcholine receptor. Like other anticholinergic (antimuscarinic) agents, it inhibits the action of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, exocrine glands and, to a limited degree, in the autonomic ganglia. Thus, it diminishes the volume and free acidity of gastric secretions and controls excessive pharyngeal, tracheal, and bronchial secretions. Glycopyrrolate antagonizes muscarinic symptoms (e.g., bronchorrhea, bronchospasm, bradycardia, and
intestinal hypermotility) induced by cholinergic drugs such as the anticholinesterases.
The highly polar quaternary ammonium group of glycopyrrolate limits its passage across lipid
membranes, such as the blood-brain barrier, in contrast to atropine sulfate and scopolamine
hydrobromide, which are highly non-polar tertiary amines which penetrate lipid barriers easily. Glycopyrrolate is marketed under the brand names Robinul, Robinul Forte, Cuvposa. In October 2015, glycopyrrolate was approved by the FDA for use as a standalone treatment for Chronic obstructive pulmonary disease (COPD), as Seebri Neohaler.
Status:
US Approved Rx
(2022)
Source:
NDA213953
(2022)
Source URL:
First marketed in 1937
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Testosterone is a steroid sex hormone found in both men and women. In men, testosterone is produced primarily by the Leydig (interstitial) cells of the testes when stimulated by luteinizing hormone (LH). It functions to stimulate spermatogenesis, promote physical and functional maturation of spermatozoa, maintain accessory organs of the male reproductive tract, support development of secondary sexual characteristics, stimulate growth and metabolism throughout the body and influence brain development by stimulating sexual behaviors and sexual drive. In women, testosterone is produced by the ovaries (25%), adrenals (25%) and via peripheral conversion from androstenedione (50%). Testerone in women functions to maintain libido and general wellbeing. Testosterone exerts a negative feedback mechanism on pituitary release of LH and follicle-stimulating hormone (FSH). Testosterone may be further converted to dihydrotestosterone or estradiol depending on the tissue. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects. Testosterone is used as hormone replacement or substitution of diminished or absent endogenous testosterone. Use in males: For management of congenital or acquired hypogonadism, hypogonadism associated with HIV infection, and male climacteric (andopause). Use in females: For palliative treatment of androgen-responsive, advanced, inoperable, metastatis (skeletal) carcinoma of the breast in women who are 1-5 years postmenopausal; testosterone esters may be used in combination with estrogens in the management of moderate to severe vasomotor symptoms associated with menopause in women who do not respond to adequately to estrogen therapy alone.
Class (Stereo):
CHEMICAL (RACEMIC)
Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
Class (Stereo):
CHEMICAL (RACEMIC)
Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
Status:
Investigational
Source:
NCT02452346: Phase 2 Interventional Completed Myelodysplastic Syndrome
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tosedostat is a proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death. There are several ongoing Phase 2 cooperative group-sponsored trials and investigator-sponsored trials evaluating the clinical activity of Tosedostat in combination with standard agents in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
Status:
Investigational
Source:
NCT02759601: Phase 1/Phase 2 Interventional Unknown status Hepatocellular Carcinoma
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tefinostat (also known as CHR-2845) was developed as an innovative oral HDAC (histone deacetylase) inhibitor that selectively targets macrophages and monocytes – central cells of the innate immune system. Chroma Therapeutics develops tefinostat for the treatment of hematological and lymphoid malignancies. In addition, the drug is under investigation in clinical trial phase I/II for cancer-associated inflammation in hepatocellular carcinoma. The aim of this study is to find the best dose of the drug without causing side effects. Besides, Phase II of clinical trial ‘MONOCLE’ study for the treatment of chronic myelomonocytic leukemia (CMML) has been initiated and the first patient has been recruited.