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A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
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The chemical name of sirolimus (also known as
rapamycin) is (3S,6R ,7E,9R ,10R,12R ,14S,15E ,17E,19E ,21S,23S ,26R,27R ,34aS)-
9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-9,27-dihydroxy-3-[(1R)-2-
[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-
hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4] oxaazacyclohentriacontine-1,5,11,28,29 (4H,6H
,31H)-pentone. Its molecular formula is C51H79NO13 and its molecular weight is 914.2.

Sirolimus is a white to off-white powder and is insoluble in water, but freely soluble in benzyl
alcohol, chloroform, acetone, and acetonitrile.
Rapamune® is available for administration as an oral solution containing 1 mg/mL sirolimus.
Rapamune is also available as a white, triangular-shaped tablet containing 1-mg sirolimus, and as
a yellow to beige triangular-shaped tablet containing 2-mg sirolimus.
The inactive ingredients in Rapamune® Oral Solution are Phosal 50 PG® (phosphatidylcholine,
propylene glycol, mono- and di-glycerides, ethanol, soy fatty acids, and ascorbyl palmitate) and
polysorbate 80. Rapamune Oral Solution contains 1.5% - 2.5% ethanol.

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