Impact of Drug Transporter Studies on Drug Discovery and Development

By nagarani - 10/31/2009

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Drug transporters are expressed in many tissues such as the intestine, liver, kidney, and brain, and play key roles in drug absorption, distribution, and excretion. The information on the functional characteristics of drug transporters provides important information to allow improvements in drug delivery or drug design by targeting specific transporter proteins. In this article we summarize the significant role played by drug transporters in drug disposition, focusing particularly on their potential use during the drug discovery and development process. The use of transporter function offers the possibility of delivering a drug to the target organ, avoiding distribution to other organs (thereby reducing the chance of toxic side effects), controlling the elimination process, and/or improving oral bioavailability. It is useful to select a lead compound that may or may not interact with transporters, depending on whether such an interaction is desirable. The expression system of transporters is an efficient tool for screening the activity of individual transport processes. The changes in pharmacokinetics due to genetic polymorphisms and drug-drug interactions involving transporters can often have a direct and adverse effect on the therapeutic safety and efficacy of many important drugs. To obtain detailed information about these inter individual differences, the contribution made by transporters to drug absorption, distribution, and excretion needs to be taken into account throughout the drug discovery and development process.

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Author : http://www.pharmainfo.net/ntakemal

Co-author : http://www.pharmainfo.net/ramamohan

discovery and development

Submitted by Pavan Kumar Alapati on Sat, 11/21/2009 - 16:20.

hi,can u give some examples regading the drug transporter studies under pipeline?

transporters

Submitted by Pavan Kumar Alapati on Sat, 11/21/2009 - 16:14.

can u specify some Multispecific Transporters?

hello

Submitted by shobha deepthik... on Fri, 11/20/2009 - 15:58.

can you tell me the recent research going on this study if you know....
In addition give a note on recently discovered drug transporters or carriers

Shobha Deepthikompella
http://www.pharmainfo.net/shobhadeepthi

query

Submitted by ROSHAN KUMAR SAHU on Fri, 11/20/2009 - 09:52.

justify"The use of transporter function offers the possibility of delivering a drug to the target organ, avoiding distribution to other organs"

References of your studies

Submitted by Amit Sharma on Fri, 11/20/2009 - 08:38.

can u give some references of ur study .....

Amit Sharma,- M.Pharm,PGDCR, (PhD)
http://www.pharmainfo.net/pharmamit

Hi Nagarani, 1.Are there any

Submitted by Y mahalaxmi on Thu, 11/19/2009 - 17:56.

Hi Nagarani,

1.Are there any models present that describe drugs interaction with drug transporters,like how we have lock and key model for describing mechanism of action of enzyme?

Thank you
Y mahalaxmi

Y Mahalaxmi
http://www.pharmainfo.net/y-mahalaxmi

Is there any therapy by which

Submitted by Ayush A. Singhal on Wed, 11/18/2009 - 17:19.

Is there any therapy by which we can induce development of new drug transporters on cell membrane?will it serve in the direction of drug effectiveness and drug resistance?

Ayush A. Singhal
RPCP, CHANGA
GUJARAT
http://www.pharmainfo.net/ayushsinghal

hello madam, my question

Submitted by Sakshi Agrawal on Wed, 11/18/2009 - 15:19.

hello madam,
my question is,how more specifically should be the drug- drug interactions taken into account during the drug developmental process...

Sakshi Agrawal
http://www.pharmainfo.net/sakshi-agrawal

Transporters and target speific drug discovery

Submitted by Sandeep Bhaskar Kale on Wed, 11/18/2009 - 12:24.

1. Can we use drug transporter studies to develop or to build informatics for target specific drug design and development? how?

Dr.Sandeep Bhaskar Kale
http://www.pharmainfo.net/sanykale123

advantages of drug transporters

Submitted by T.Nithya on Sun, 11/15/2009 - 16:05.

hi
naga rani
good presentation
can u please explain the advantages of drug transporters,and some examples

http://www.pharmainfo.net/nithya035

classify the families of different types of transporters?

Submitted by Ritesh Bajaj on Sat, 11/14/2009 - 11:23.

hello mam,

How can you classify the families of different types of transporters?

difference between primary & secondary active transporters?

Submitted by Bhawna Khurana on Sat, 11/14/2009 - 09:50.

hello mam,

can you please tell me the difference between primary & secondary active transporters?

HY........ HOW DRUG-DRUG

Submitted by komal nikam on Thu, 11/12/2009 - 13:27.

HY........

HOW DRUG-DRUG INTERACTION AFFECT ON A.D.M.E.OF TRANSPORTER,PLEASE EXPLAIN WITH THE HELP OF TRANSPORTER WHICH IS ABLE TO CROSS BBB?

Komal Nikam
http://www.pharmainfo.net/komal-nikam

HY NAGARANI, CAN U PLEASE

Submitted by komal nikam on Thu, 11/12/2009 - 13:25.

HY NAGARANI,

CAN U PLEASE ELABORATE THE PRAVASTATIN & ITS DERIVATIVE AS THE TRANSPORTER?WHICH DIFFICULTIES OCCUR IN ITS EXCRETION?

REGARDS,
KOMAL

Komal Nikam
http://www.pharmainfo.net/komal-nikam

Can we use drug transporters to study food-drug interactions?

Submitted by Dr. T.E.G.K. Murthy on Thu, 11/12/2009 - 06:12.

1. Can we use drug transporters to study food-drug interactions?

2. Whether the distribution of drugs is influenced by transporters or not?

Transporter localization!!

Submitted by Jithan Aukunuru on Thu, 11/12/2009 - 00:48.

HI,

what is the importance of transporter localization in the pharmacokinetics of drug substances?

toxicity

Submitted by Amol S. Malpani on Mon, 11/09/2009 - 16:04.

Dear Nagarani,
How drug transporters are affecting toxicity in body?
Next time try to reduce matter per slide.
Regards,
Amol

Amol
http://www.pharmainfo.net/amolsmalpani

Co-administration of erythromycin and Talinolol

Submitted by Bhasker on Fri, 11/06/2009 - 16:00.

Hi Nagarani,
one of your slides represented that Co-administration of erythromycin increased the absorption of Talinolol due to P-gp inhibition by Erythromycin.
My question is what is the normal dosing range to inhibit P-gp.Is it sub-therapeutic or Therapeutic?
If it is therapeutic range than we would face the side effects of erythromycin prior to P-gp inhibition.let me know your comments about this.

Bhasker
http://www.pharmainfo.net/bhasker

Genome based drug discovery

Submitted by Dixon Thomas on Wed, 11/04/2009 - 02:27.

Yes Nagarani
The genome based drug discovery will be popular as there will be more genomes recognized as drug receptors (where the drug finally bind or react to shoe the pharmacological action). Do you have information about any proved genome drug receptors?

Mr. Dixon Thomas, M. Pharm, M. S., RPh
http://www.pharmainfo.net/pharmacistdixon

OAT1,OATP,NTCP,OCT,OCTN,PEPT,MRP2,MDR1,BCRP

Submitted by shobha deepthik... on Mon, 11/02/2009 - 15:50.

Hey can u please explain in detail.the folllowing.. as u have not given the full form of the following abbreviated forms...
OAT1,OATP,NTCP,OCT,OCTN,PEPT,MRP2,MDR1,BCRP..........
U failed to explain those in your ppt.......
IN ADDITION CAN YOU PLEASE LET ME KNOW........What is the fate of by other transporters in other body parts oterthan in kidney....plz explain....
finally tell me about some which are in clinical trials which are experimented to be carried by different transporters..

With best wishes,
shobha deepthi.