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Status:
US Approved Rx
(2006)
Source:
ANDA077552
(2006)
Source URL:
First approved in 1977
Source:
TOPICORT by TARO
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Desoximetasone (Topicort®) is a topical anti-inflammatory glucocorticoid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses and for the treatment of plaque psoriasis in patients 18 years of age or older. The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. They play a role in cellular signaling, immune function, inflammation and protein regulation; however, the precise mechanism of action in psoriasis is unknown. The mechanism of anti-inflammatory activity of the topical corticosteroids is also unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man.
Status:
US Approved Rx
(1977)
Source:
NDA017765
(1977)
Source URL:
First approved in 1977
Source:
NDA017765
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Clocortolone (used in form of pivalate prodrug) is a topical glucocorticoid that was approved by FDA for the treatment of corticosteroid-responsive skin disorders. The drug exerts its anti-inflammatory action by binding to glucocorticoid receptor which results in regulation of the expression of proinflammatory cytokines and further antiproliferative, immunosuppressive, and initial vasoconstrictive effects.
Status:
US Approved Rx
(2023)
Source:
ANDA214814
(2023)
Source URL:
First approved in 1977
Source:
NDA017422
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Carmustine is a cancer medication that interferes with the growth and spread of cancer cells in the body. Carmustine is used to treat brain tumors, Hodgkin's disease, multiple myeloma, and non-Hodgkin's lymphoma. Although it is generally agreed that carmustine alkylates DNA and RNA, it is not cross-resistant with other alkylators. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins. Pulmonary toxicity characterized by pulmonary infiltrates and/or fibrosis has been reported to occur from 9 days to 43 months after treatment with BiCNU and related nitrosoureas. A frequent and serious toxicity of BiCNU is delayed myelosuppression. Nausea and vomiting after intravenous administration of BiCNU are noted frequently. Greater myelotoxicity (e.g., leukopenia and neutropenia) has been reported when carmustine was combined with cimetidine.
Status:
US Previously Marketed
Source:
DIDRONEL by MGI PHARMA INC
(1987)
Source URL:
First approved in 1977
Source:
DIDRONEL by APIL
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Etidronate is a salt of etidronic acid (brand name Didronel, also known as EHDP) a diphosphonate, which is indicated for the treatment of symptomatic Paget’s disease of bone and in the prevention and treatment of heterotopic ossification following total hip replacement or due to spinal cord injury. Didronel is not approved for the treatment of osteoporosis. This drugs acts primarily on bone. It can inhibit the formation, growth, and dissolution of hydroxyapatite crystals and their amorphous precursors by chemisorption to calcium phosphate surfaces. Inhibition of crystal resorption occurs at lower doses than are required to inhibit crystal growth. Both effects increase as the dose increases. Preclinical studies indicate etidronate disodium does not cross the blood-brain barrier. Didronel is not metabolized. The amount of drug absorbed after an oral dose is approximately 3 percent. Bisphosphonates, when attached to bone tissue, are absorbed by osteoclasts, the bone cells that breaks down bone tissue. Although the mechanism of action of non-nitrogenous bisphosphonates has not been fully elucidated, available data suggest that they bind strongly to hydroxyapatite crystals in the bone matrix, preferentially at the sites of increased bone turnover and inhibit the formation and dissolution of the crystals. Other actions may include direct inhibition of mature osteoclast function, promotion of osteoclast apoptosis, and interference with osteoblast-mediated osteoclast activation. Etidronic acid may promote osteoclast apoptosis by competing with adenosine triphosphate (ATP) in the cellular energy metabolism. The osteoclast initiates apoptosis and dies, leading to an overall decrease in the breakdown of bone.
Status:
US Previously Marketed
Source:
LORELCO by SANOFI AVENTIS US
(1977)
Source URL:
First approved in 1977
Source:
LORELCO by SANOFI AVENTIS US
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Probucol is used to lower levels of cholesterol (a fat-like substance) in the blood. Probucol is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. This may help prevent medical problems caused by cholesterol clogging the blood vessels. Probucol was voluntarily removed from the market in the United States during 1995. The withdrawal from the market was due to safety concern. robucol lowers serum cholesterol by increasing the fractional rate of low-density lipoprotein (LDL) catabolism in the final metabolic pathway for cholesterol elimination from the body. Additionally, probucol may inhibit early stages of cholesterol biosynthesis and slightly inhibit dietary cholesterol absorption. Recent information suggests that probucol may inhibit the oxidation and tissue deposition of LDL cholesterol, thereby inhibiting atherogenesis. It appears to inhibits ABCA1-mediated cellular lipid efflux.
Status:
US Previously Marketed
Source:
OPTIMINE by SCHERING
(1977)
Source URL:
First approved in 1977
Source:
OPTIMINE by SCHERING
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Azatadine is an antihistamine, which blocks the effects of the naturally occurring chemical histamine in the body. Azatadine is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; and other symptoms of allergies and the common cold. The antihistamines antagonize those pharmacological effects of histamine, which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Status:
US Previously Marketed
Source:
ESTROVIS by PARKE DAVIS
(1977)
Source URL:
First approved in 1977
Source:
ESTROVIS by PARKE DAVIS
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Quinestrol is a synthetic estrogen that is effective in hormone replacement therapy. It is a 3-cyclopentyl ether of ethynyl estradiol. After gastrointestinal absorption, it is stored in adipose tissue, where it is slowly released and metabolized in the liver to its active form, ethinyl estradiol. Quinestrol has found limited use in suppressing lactation in postpartum women and, in combination with synthetic progestogens, as contraceptive therapy, although additional studies are needed for both applications. Estrogens diffuse into their target cells and interact with a protein receptor (the estrogen receptor). Estrogen interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).
Status:
Possibly Marketed Outside US
First approved in 1977
Source:
NADA128620
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Fenbendazole (FBZ) is a broad-spectrum benzimidazole antiparasitic drug currently approved for use in numerous animal species, including rodents. Although nematodes, and in particular pinworms, are the main endoparasites of concern in laboratory rodents, FBZ also is indicated for use in other animal species against a wide spectrum of nematodes, tapeworms, flukes, and protozoa (Giardia duodenalis, Encephalitozoon intestinalis). The molecular mode of fenbendazole action consists in binding of beta-tubulin monomer prior to dimerisation with alfa-tubulin which blocks subsequent microtubule formation. These microtubules are important organelles involved in the motility, the division and the secretion processes of cells in all living organisms. In the worms the blocking of microtubules perturbs the uptake of glucose, which eventually empties the glycogen reserves. This blocks the whole energy management mechanism of the worms that are paralyzed and die or are expelled. FBZ have a greater binding to nematode as compared to mammalian tubulin at 37°C. The oral LD50 of p-OH fenbendazole was >10 000 mg/kg b.w. in mice and rats.
Status:
Possibly Marketed Outside US
First approved in 1977
Source:
NDA021777
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Diethyl phthalate is a colourless liquid with a slight aromatic odour and low volatility. Diethyl phthalate is used as a plasticizer for
cellulose ester plastic films and sheets (photographic, blister packaging, and tape applications) and moulded and extruded articles (consumer articles such as toothbrushes, automotive components, tool handles, and toys). Diethyl phthalate was reported as an ingredient in 67 cosmetic formulations. Diethyl phthalate is used as a component in insecticide sprays and mosquito repellents. Diethyl phthalate is likely to undergo biodegradation in the environment. General population exposure in the USA, as estimated from urinary concentrations of the monoester, was estimated to be 12 µg/kg body weight per day (median value). Dermally applied diethyl phthalate penetrates the skin and can be widely distributed in the body, but it does not accumulate in tissue. Diethyl phthalate has irritant effects on the eyes, skin, and mucous membranes and can lead to central nervous system (CNS) effects in exposed workers. The exposure to diethyl phthalates (DEP), a parent compound of the monoethyl phthalate (MEP) metabolite, may be associated with increased risk of BC (Odds Ratio of 2.20, p value for trend, p<0.003).
Status:
Possibly Marketed Outside US
Source:
M032
(2017)
Source URL:
First approved in 1977
Source:
21 CFR 333C
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Lauramide DEA is a compound made from a saturated fatty acid called lauric acid and diethanolamine or DEA, an ingredient in some cosmetic products that functions as a wetting agent. Combinations of fatty acids and DEA like lauramide DEA are referred to as diethanolamides. The diethanolamide lauramide DEA is an ingredient in some personal care products including shampoo, hair coloring products, hand soap, bubble baths, bath gels and lotions. In cosmetic and personal care products, lauramide DEA enhances a product’s ability to form and maintain foam. It also increases the viscosity or thickness of products. This gives them a more substantial feel. Without a viscosity-enhancing agent, shampoos and other personal care products would be considered too “runny” by some. Viscosity increasing agents like lauramide DEA are often combined with surfactants to maximize the texture and performance of cosmetic and personal care products that foam like shampoo and bubble bath. Lauramide DEA also serves as an emulsion stabilizer that helps to keep water-soluble and oil-soluble ingredients together in a product. Diethanolamides like lauramide DEA are found in cosmetic and personal care products in concentrations of between 1 and 10%. At these concentrations, the Cosmetic Ingredient Review Expert Panel, a group of independent experts that looks at the safety of cosmetic ingredients, deems lauramide DEA to be safe. This assumes that lauramide DEA isn’t contamined with other ingredients called nitrosating agents. Nitrosating agents interact with lauramide DEA to form nitrosamines, chemicals linked with an increased risk of cancer. This can happen during the manufacture of a product or during storage. Such ingredients must be excluded from products that contain diethanolamides like lauramide DEA, although there are still concerns about contamination. Topically, lauramide DEA can cause mild skin irritation. There are also reports of contact dermatitis and allergic reactions in some people.