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Status:
US Previously Marketed
Source:
TRIKETOL DEHYDROCHOLIC ACID by ENDO
(1961)
Source URL:
First marketed in 1935
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Sodium dehydrocholate is a hydrocholeretic and is used to study biliary excretion.
Status:
US Previously Marketed
Source:
Chrysarobin U.S.P.
(1921)
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Chrysarobin was originally extracted from Goa powder, a substance deposited in the wood of Andira Araroba, Aguiar (Nat. Ord.—Leguminosae). Chrysarobin (1,8-dihydroxy-3-methyl-9-anthrone) has enol tautomer of 1,8,9-trihydroxy-3-methyl-anthracene. Chrysarobin exerts antipsoriatic action. The use of chrysarobin has a number of quite serious disadvantages, not the least of which is that it can result in severe staining and irritation of the skin. Chrysarobin is an anthrone skin tumor promoter.
Status:
Possibly Marketed Outside US
Source:
Unknown by I.G. Farbenindustrie
Source URL:
First approved in 2018
Source:
21 CFR 358H
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor, that has been used for psoriasis vulgaris and acne treatment. Tioxolone is reported to possess cytostatic, antipsoriatic, antibacterial and anti-mycotic properties. Tioxolone is also added to some cosmetics (e.g. hair shampoos and skin cleansers), due to claims for its oil-regulating and antibacterial properties.
Status:
Possibly Marketed Outside US
Source:
ROBENGATOPE by Photogen Technologies
Source URL:
First approved in 2013
Source:
GloStrips by Nomax Inc.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Rose bengal sodium (RB) is a small molecule, halogenated xanthene being developed by Provectus Biopharmaceuticals (formerly Provectus Pharmaceuticals). It is commonly used in eye drops to stain damaged conjunctival and corneal cells and thereby identify damage to the eye. The stain is also used in the preparation of Foraminifera for microscopic analysis, allowing the distinction between forms that were alive or dead at the time of collection. A form of rose bengal is also being studied as a treatment for certain cancers and skin conditions. The cancer formulation of the drug, known as PV-10, is currently undergoing clinical trials for melanoma and breast cancer. Recently, interest in RB as a therapeutic cancer treatment has increased due to significant anti-tumor responses with direct tumor injection in human clinical trials for metastatic melanoma. In these patients, there has been the implication that RB may mount a T-cell mediated anti-tumor response and impart antigen-specific responses in distant bystander lesions.
Status:
Possibly Marketed Outside US
Source:
Prosoria Psoriasis Treatment by General Foods
Source URL:
First approved in 2012
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tetrahydrodiferuloylmethane (aka Tetrahydrocurcumin) is a bioactive metabolite of curcumin. It has been shown to have anti-inflammatory, anti-oxidant, anti-cancer, and neuroprotective effects in several in vitro and in vivo models. However, there have been no advances in human trials for these conditions. It should be noted that tetrahydrocurcumin is used in non-medicinal skin care formulations intended for skin whitening, skin soothing, and anti-oxidant effects.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Talcalcitol is a synthetic analogue of vitamin D3. Tacalcitol has been developed by Teijin in Japan with the aim of maintaining the potent cell-regulating properties of calcitriol without the calcium-related adverse effects. Tacalcitol differs structurally from calcitriol by hydroxylation in the 24 position instead of the 25 position. Tacalcitol can influence the principal pathogenetic factors of psoriasis by inducing normalisation of keratinocyte differentiation, performing an anti-proliferative action and finally modulating the inflammatory response. Tacalcitol has been launched as an ointment formulation for the treatment of psoriasis in various countries. High-dose formulations (ointment and lotion) are available in Japan.
Status:
Possibly Marketed Outside US
Source:
ProZ92 by Liebermann, C.|Seidler, P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
9-Hydroxy chrysarobin or 3-methylanthralin is a pure product of chrysophanic acid reduction. The compound 3-methylanthralin is listed in the Merck Index as an antipsoriatic. Chrysarobin is a mixture of compounds derived from Goa powder, and includes 3-methylanthralin. Goa powder (Araboba) is derived from the wood and bark of Andria Araroba Aguiar (Leguminosae). Literature references describing the isolation of chrysarobin date back to the second part of 1800s. A method of reducing chrysarobin to obtain 3-methylanthralin was known as early as 1931. At present chrysarobin is used in the topical antipsoriatic compositions with natural plant extracts and as a homeopatic product. Pure 3-methylanthralin when tested on mice in vivo was found to play an important role in skin hyperplasia and promotion of skin carcinogenesis by effecting the expression of several gap-junctional proteins connexins (Cxs) and inhibiting glucocorticoid receptor expression in mouse epidermis specifically in keranocytes. Chrysarobin is approved by FDA as an over-the-counter drug. ProZ92 is a trade name a patented botanical formula, topical marketed in Israel which primary anti-psoriatic agents are: 3-methylanthralin, chrysophanol, aloe-emodin and aloe-emodin acetate.
Status:
Possibly Marketed Outside US
Source:
Dovonex by Leo Pharma
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
MC-1046 (Impurity A of Calcipotriol) is the C22-23-unsaturated 24-ketone, an active metabolite of the synthetic vitamin D analog calcipotriol (calcipotriene, MC 903). Calcipotriene is a ligand of VDR-like receptors approved for topical dermatological use indicated for the treatment of plaque psoriasis. It is approved by FDA in United States under the trade name Dovonex. Calcipotriol displays minimal effects on calcium homeostasis, and regulates cell differentiation, and proliferation exhibiting antiproliferative activity against human HL-60, HL60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines. Calcipotriol is an effective anti-proliferative agent when applied topically at high concentrations but it is relatively “noncalcemic” in vivo (administered perorally, intravenously or intraperitoneally) because it can be metabolized by a variety of cells to metabolites with reduced biological activity as was demonstrated in vitro using rat and human cell lines from liver, bone, kidney, and keratinocytes. MC1046 is the initial calcipotriol metabolite which concentration reaches a steady state after 4 h of incubation with cells in vitro whereas the concentration of another major MC 903 metabolite MC1080, C22-23-saturated 24-ketone, continues to increase linearly over the time period tested (20 h). These two metabolites have also been detected in vivo in serum from rats and pigs dosed with MC903. MC1046 has the ability to stimulate e VDRE-mediated human growth hormone production in COS-1 cells co-transfected with pSG5hVDR1/3 and (CT4)4TKGH vectors and also binds to VDR although with lower (1/133) binding affinity compared to calcipotriol.
Status:
Possibly Marketed Outside US
Source:
NCT02200978: Phase 4 Interventional Completed Childhood Acute Promyelocytic Leukemia
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Indirubin is derived from the Indigo Plant (Isatis Root, Isatis Leaf). It is used as part of a traditional Chinese herbal prescription called Dang Gui Long Hui Wan, to treat chronic myelogenous leukemia (CML). Indirubin inhibits DNA synthesis in several cell lines, in a cell-free assay and in vivo in rats with Walker-256 sarcoma. A weak binding of indirubin to DNA in vitro has been described. Indirubin inhibited all cyclin-dependent kinases (1,2,4,5) almost equally. Indirubin has been approved for clinical trials against chronic myelocytic and chronic granulocytic leukaemia. A few studies show that Indirubin is effective against psoriasis. Mild to severe nausea, vomiting, abdominal pain, diarrhea, headache, and edema are reported adverse events of Indirubin. Long-term oral ingestion has also occasionally been associated with hepatitis, pulmonary arterial hypertension and cardiac insufficiency.
Status:
Possibly Marketed Outside US
Source:
FUMADERM
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ethyl fumarate is an anti-psoriatic agent. Its salts are used for the treatment of severe psoriasis (Fumaderm formulation). The mechanism of its action is unknown.