药物动力学和代谢formestane的乳腺癌患者。

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朗PE、聊聊J, Johannessen特区Gschwind惠普,Waldmeier F,施耐德W,加利B,温克勒T,布卢姆W, Kriemler惠普,米勒WR, Faigle JW

药物动力学和代谢formestane的乳腺癌患者。

J类固醇生物化学杂志。2001年4月,77 (1):39-47。

PubMed ID

11358673 (在PubMed

]

文摘

Formestane (Lentaron (R)、4-hydroxyandrostenedione)甾类芳香化酶抑制剂用于治疗晚期乳腺癌。临床上,管理仓库形式一旦双周刊,肌内注射(坜)。探讨药物动力学、生物利用度和药物的代谢,7个患者接受单剂量250毫克贝聿铭商业formestane天0,21岁,35岁,49和63年的试验。63天,三个患者接受额外的单一静脉(注射)脉冲剂量的1毫克的14 c-labelled formestane。等离子体动力学后即时定量确认网站的持续释放formestane注入。在24 - 48 h的第一剂量,循环药物达到C (max) 48.0 + / - -20.9 nmol / l(意思是+ /南达科他州。N = 7)。结束时给药间隔,14天后,血浆浓度仍为2.3 + / - -1.8 nmol / l。动力学变量没有显著改变在长期治疗。肌内剂量似乎完全生物利用率。 Following i.v. injection of 14C-formestane, the unchanged drug disappeared rapidly from plasma, the terminal elimination half-life being 18+/-2 min (N=3). Plasma clearance, CL was 4.2+/-1.3 l/(h kg) and the terminal distribution volume V(z) was 1.8+/-0.5 l/kg. The drug is mainly eliminated by metabolism, renal excretion of metabolites accounting for 95% of dose. The excretory balance of 14C-compounds in urine and faeces totals up to 98.9+/-0.8% of the i.v. dose after 168 h. The 14C-compounds in plasma and urine were separated by HPLC, and three major metabolites were submitted to structural analysis by MS, NMR and UV spectroscopy. One of the metabolites is the direct 4-O-glucuronide of formestane. The other two represent 3-O-sulfates of the exocons 3beta,4beta-dihydroxy-5alpha-androstane-17-one and 3alpha,4beta-dihydroxy-5alpha-androstane-17-one, their ratio being 7:3. These exocons are formed by stereoselective 3-keto reduction, accompanied by reduction of the 4,5-enol function. The exocons do not inhibit human placental aromatase activity in vitro.

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药物

Formestane