RE: enzyme turnover

From: James G Wright Date: February 15, 2008 technical Source: mail-archive.com
There are no measurement in A(3), therefore there are no units. The steady-state amount can be any arbitrary value, as all changes are relative. Set A_0(3)=1, and KENZ=KIN=KOUT, and KENZ/KENZ=1. KENZ determines the half-life, and is the only quantity the can be estimated without direct data. If the code isn't working, the most likely case is that there is a clearance process that is not mediated by the destructible enzyme, and therefore the amount going into the metabolite compartment may depend on the dose administration schedule. There are a lot of possible problems in parent-metabolite models which can be difficult to unravel due to the uncertain input of metabolite. The metabolite could require more than one compartment, or first-pass formation (possibly saturable) of metabolite may need to be included in the model. Best regards, James James G Wright PhD Scientist Wright Dose Ltd Tel: 44 (0) 772 5636914
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-----Original Message----- From: [EMAIL PROTECTED] [mailto:[EMAIL PROTECTED] On Behalf Of Magnusson, Mats Sent: 15 February 2008 11:26 To: Khaled Nm; [email protected] Subject: RE: [NMusers] enzyme turnover Khaled, I agree with John, you will in this case need a separate production rate term (RIN) and state that A_0(3) = RIN / KENZ, and then let CL24 change by A(3)/A_0(3). Depending on the mechanism of the inhibition, you might consider adding -KIRR*C2*A(3) (after being transformed to only masses or concentrations) to DADT(2). /Mats Mats Magnusson, PhD Pharmacometrician Pfizer Global Research & Development Sandwich, Kent CT13 9NJ UK Khaled, You seem need another parameter. KENZ cannot be both a creation and a death rate for A(3) (i.e. [mg/h] and [1/h]). Also, it is confusing the way you use both masses and concentrations in your interaction terms. Do you intend CL24 to be L h-1 mg-1? John John C Lukas Strategic Consulting Services Pharsight Corp. line: + 33 492 726 495 cell: + 33 626 496 777 _____ From: [EMAIL PROTECTED] [mailto:[EMAIL PROTECTED] On Behalf Of Khaled Nm Sent: Wednesday, February 13, 2008 2:08 PM To: [email protected] Subject: [NMusers] enzyme turnover Dear nmuser, I had analyzed data set of a CYP- inhibitor agent using NONMEM ADVAN 6. A two-comp. model was used to describe the parent and its metabolite data sets sid by side to a hypothetical enzyme compartment. All estimates are fine except the KENZ (enzyme turnover rate was about (2 hr-1) which is 100-fold the published value. my code is $DES C2=A(2)/V2 ; for parent C4=A(4)/V4 ; for metab DADT(1)= -KA*A(1) DADT(2)=KA*A(1) - CL24*A(3)*C2 DADT(3)= KENZ - KENZ*A(3) - KIRR *C2 *A(3) DADT(4)=CL24*A(3)*C2 - CL40*C4 If i use the Emax and IC50 mode, the result is similar. what is wrong with my code ? All suggesion are wellcome. Regards Khaled _____ Be a better friend, newshound, and know-it-all with Yahoo! Mobile. Try http://us.rd.yahoo.com/evt=51733/*http:/mobile.yahoo.com/;_ylt=Ahu06i62 sR8HDtDypao8Wcj9tAcJ%20 it now.
Feb 13, 2008 Khaled Nm enzyme turnover
Feb 15, 2008 John Lukas RE: enzyme turnover
Feb 15, 2008 Mats Magnusson RE: enzyme turnover
Feb 15, 2008 James G Wright RE: enzyme turnover