ライフサイエンスコーパス: intrinsic clearance

1 m and exhibited metabolic stability with low intrinsic clearance.

2 ayed improved oral bioavailability and lower intrinsic clearance.

3 Despite its high in vitro metabolic intrinsic clearance, 23r (AMG 900) showed acceptable pha

4 , it was depleted by CYP26A1 (Km = 63 nM and intrinsic clearance = 90 mul/min per pmol).

5 Epelsiban has low levels of intrinsic clearance against the microsomes of four speci

6 d AVI-6451, a potent Mac1 inhibitor with low intrinsic clearance and high oral bioavailability that a

7 e-NH2 resulted in high affinity and improved intrinsic clearance and intestinal epithelial permeabili

8 Further mitigation of human intrinsic clearance and time-dependent inhibition led to

9 75 displayed excellent microsomal stability, intrinsic clearance, and hepatic extraction ratios with

10 In this article, we describe an in vitro intrinsic clearance-based approach to the optimization o

11 trinsic clearance to a prediction of in vivo intrinsic clearance by reconciling the enzymatic content

12 bioconcentration factor (BCF), the in vitro intrinsic clearance (CL(IN VITRO,INT)) from rainbow trou

13 The estimated in vitro intrinsic clearance (Clint) of TBECH mixture was slower

14 These compounds have significantly reduced intrinsic clearance compared to our initial series of py

15 hile increasing polarity in order to improve intrinsic clearance culminated with the discovery of pur

16 Measured rates of intrinsic clearance determined using cryopreserved trout

17 ty-purified liver GST and GST-alpha 1-1, the intrinsic clearance for busulfan conjugation was 0.87 an

18 In vitro intrinsic clearances for CYP2C9*5, calculated as the rat

19 to values predicted from published in vitro intrinsic clearances for validation of IVIVE models.

20 vatives with low cynomolgus monkey and human intrinsic clearance gave 2',6'-dimethyl-3'-pyridyl R-sec

21 ges the common approach of screening for low intrinsic clearance in vitro to target high unbound expo

22 Instead, low intrinsic clearance leads to high in vivo unbound plasma

23 Cell-intrinsic clearance occurred in cell culture, too, with

24 previous study with determination of hepatic intrinsic clearance of (1)(8)F-FDGal (V*(max/K*(m)).

25 bility assay revealed high stability and low intrinsic clearance of 17d (T(1/2) > 145 min and CL(int(

26 In HRN mice the in vitro metabolism and intrinsic clearance of CPA was over 6-fold lower than in

27 val kinetics of galactose, including hepatic intrinsic clearance of galactose (V(max)/K(m)) from meas

28 The intrinsic clearance of glutamate was reduced by 12.3-fol

29 and 6.2-fold (S457F, P < 0.01), whereas the intrinsic clearance of methotrexate was reduced by 4.2-f

30 tudy, three laboratories determined in vitro intrinsic clearance of six reference compounds (benzo[a]

31 me P450 (CYP) enzymes is responsible for the intrinsic clearance of the majority of therapeutic drugs

32 To test if the higher intrinsic clearance of type II binding compounds relativ

33 ytes can be used to reliably obtain in vitro intrinsic clearance of xenobiotics, which provides suppo

34 ed in preclinical models, but the high human intrinsic clearance precluded further development and pr

35 ed in preclinical models, but the high human intrinsic clearance precluded further development and pr

36 etabolism in vitro, scaling-up this in vitro intrinsic clearance to a prediction of in vivo intrinsic

37 tory variability (% CV) in measured in vitro intrinsic clearance values ranged from 4.1 to 30%, while

38 The intrinsic clearance (Vmax/K(m)) of busulfan conjugation

39 )C-CSar from blood to bile, as quantified by intrinsic clearance, was significantly lower in experime

40 By lowering the intrinsic clearance, we derived a set of imidazobenzoxaz

41 a stability but approximately 3-fold greater intrinsic clearance when compared to olaparib.