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Thymidylate synthase

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1971

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Candida endocarditis

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Hoffman-La Roche

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FLUCYTOSINE

D83282DT06

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Status:

US Approved Rx (1971)

First approved in 1971

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Thymidylate synthase

Thymidylate synthase

Conditions:

Systemic candidiasis

Cryptococcal meningitis

Cryptococcus pulmonary infections

Candida urinary system infections

Candida endocarditis

Flucytosine (5-flucytosine, Ancobon) is an antifungal agent used for treatment of serious fungal infections caused by Candida or Cryptococcus. A fluorinated cytosine analog it was originally developed as an anti-tumor agent, but was found to be non-e...

ffective against tumors. Monotherapy with 5-FC is limited because of the frequent development of pathogens resistance. It is often used in in combination with amphotericin B. The severe side effects of 5-flucytosine include hepatotoxicity and bone-marrow depression. 5-fluorocytosine is a prodrug to the cytotoxic compound 5-fluorouracil. Although the exact mode of action is unknown, it has been proposed that flucytosine acts directly on fungal organisms by competitive inhibition of purine and pyrimidine uptake and indirectly by intracellular metabolism to 5-fluorouracil. Flucytosine is taken up by fungal organisms via the enzyme cytosine permease. Inside the fungal cell, flucytosine is rapidly converted to fluorouracil by the enzyme cytosine deaminase. Fluorouracil exerts its antifungal activity through the subsequent conversion into several active metabolites, which inhibit protein synthesis by being falsely incorporated into fungal RNA or interfere with the biosynthesis of fungal DNA through the inhibition of the enzyme thymidylate synthetase.

4-BROMOPHENETOLE

T0L17BX1WR

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

O-XYLYL BROMIDE

3NDQ4L309U

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

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