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Pyronin Y is an intercalating dye with a specificity towards RNA. It has been shown to accumulate in the mitochondria of viable cells. Pyronin Y has been used to measure RNA in flow cytometry. Pyronin Y possesses some anti-cancer properties: it causes cell cycle arrest and increases lifespan in a mouse model of sarcoma.
Status:
US Previously Marketed
First marketed in 1919
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.
Status:
US Approved Rx
(2015)
Source:
NDA208169
(2015)
Source URL:
First approved in 2015
Source:
NDA208169
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Uridine triacetate (formally PN401) is an acetylated prodrug of uridine. Following oral administration, uridine triacetate is deacetylated by nonspecific esterases present throughout the body, yielding uridine in the circulation. Uridine triacetate under VISTOGARD trade name is a uridine replacement agent approved for the emergency treatment of fluorouracil or capecitabine overdose (regardless of the presence of symptoms) or early-onset severe or life-threatening cardiac or central nervous system (CNS) toxicity and/or early-onset unusually severe adverse reactions (eg, gastrointestinal [GI] toxicity and/or neutropenia) within 96 hours following the end of fluorouracil or capecitabine administration in adult and pediatric patients. Uridine competitively inhibits cell damage and cell death caused by fluorouracil. Fluorouracil is a cytotoxic antimetabolite that interferes with nucleic acid metabolism in normal and cancer cells. Cells anabolize fluorouracil to the cytotoxic intermediates 5-fluoro-2’-deoxyuridine-5’- monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits thymidylate synthase, blocking thymidine synthesis. Thymidine is required for DNA replication and repair. Uridine is not found in DNA. The second source of fluorouracil cytotoxicity is the incorporation of its metabolite, FUTP, into RNA. This incorporation of FUTP into RNA is proportional to systemic fluorouracil exposure. Excess circulating uridine derived from VISTOGARD is converted into uridine triphosphate (UTP), which competes with FUTP for incorporation into RNA. Uridine triacetate is also approved for the treatment of hereditary orotic aciduria under XURIDEN trade name. Uridine triacetate provides uridine in the systemic circulation of patients with hereditary orotic aciduria who cannot synthesize adequate quantities of uridine due to a genetic defect in uridine nucleotide synthesis.
Status:
US Approved Rx
(2018)
Source:
ANDA209365
(2018)
Source URL:
First approved in 1998
Source:
NDA020896
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug which is converted to 5-fluorouracil (5-FU). Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis. Most common adverse reactions (≥30%) were diarrhea, hand-and-foot syndrome, nausea, vomiting, abdominal pain, fatigue/weakness, and hyperbilirubinemia. The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin.
Status:
US Previously Marketed
First marketed in 1919
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.
Status:
US Previously Marketed
First marketed in 1919
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.
Status:
US Previously Marketed
First marketed in 1919
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.
Status:
US Previously Marketed
First marketed in 1919
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.