REVIEW ON THE LEAD OPTIMIZATION TECHNIQUES (PHASE-I)

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About Authors:
Kambham Venkateswarlu*, D.Z.Suhasini
Department of Pharmacology,
Sri Lakshmi Narasimha College of Pharmacy (JNTUA), Pallur,
Chittoor, Andhra Pradesh, India.
*k.v.reddy9441701016@gmail.com

ABSTRACT:
Lead optimization techniques are deals that new discovery is to choose the compounds with a known pharmacological action and proceed to modify the molecular structure of the compound systemically to get a drug with desired properties pharmacological action and pharmacokinetics. The compounds of the drugs are choosing for the study is called as lead.

Generally the identification and synthesis of compounds which are structurally related to the lead compound and testing their pharmacological activity. In the process it is possible to find a better drug than the lead compound.

Reference Id: PHARMATUTOR-ART-1530

I. INTRODUCTION:
The discovery and development of a new drug is a complex process, full of hidden obstacles.

In order to respond to the great variety of therapeutic needs and meet national and international regulatory requirements, these processes, which themselves demand an integrated multi disciplinary approach, must be conducted with absolute scientific rigor.

The discovery and development of a new drug can take between 7 and 15 years and experts estimate the average cost to be $us802m (2000).

The structure of the lead compound is modified by synthesizing the analogue, to amplify the desired activity and to minimize or eliminate the unwanted properties.

II.BASIC PRINCIPLE:
The basic principles in the discovery and development of a drug may be summarized as follows:

2.1 Discovery:
The discovery stage can last up to 6 years and experts estimate its average cost to be US335m (2000).

The proteins produced by transcription of our genes ensure that our body’s main biological functions are carried out.

A faulty gene or protein is often what lies behind a disease.

To treat a particular disease, it is first necessary to identify the biological targets (i.e., a protein or other biopolymer) known to be involved in this disease’s etiology and then discover the compound or compounds that have an effective and specific therapeutic capability and a minimum number of side effects.

Specialists in the biological-sciences and medicinal chemistry work in close collaboration throughout the entire process of drug discovery.

2.3 Development:
The development of the drug can take as long as a decade at an average cost estimated at $us467m (2000).

Once the compound or compounds have been chosen, they must be transformed into a drug this process involves several series of trials on animals and humans, all intended to ensure that the drug may be administered to humans with minimum possible risk and that it is superior to or otherwise complements existing drugs with the same therapeutic function.

These trials are subject to the rigorous controls required by the regulatory authorities such as Health-Canada or the US Food and Drug Administration (FDA).

In addition to specialists in biology and therapeutic chemistry, the discovery of a new drug involves the collaboration of pharmaceutical R&D specialists and clinical research teams, composed of doctors, nurses and other health specialists.

2.4 The Discovery and Development of a New Drug over View:

Experts estimate the cost of the development of a new drug to be $us802m (2000). This amount includes expenses related to the interrupted development of molecules that failed to meet specific characteristics required for commercialization. It also includes the cost of capital investments.

III. TARGET IDENTIFICATION / VALIDATION:

Duration:  From several months to several years

In order to ensure the successful development of new drugs the pharmaceutical industry requires considerable scientific and financial resources must from the strategic alliances with industrial pertness the university research community and companies conducting research under contract drugs that act in new ways upon biological targets specific to the diseases requiring new therapeutic approaches.

Thus identification of therapeutic targets requires knowledge of diseases etiology and the biological systems are associated with it.

Recent findings issuing from the “human genome” project have seen the odyssey of drug discovery become very sophisticated indeed. Over the last 50 years most of the drugs commercialized were developed for around 500 known biological targets now, the many projects involved in the study of the “genome and proteome” of humans and other organisms are beginning to contribute to the discovery of new biologically interesting targets.

IV. LEAD IDENTIFICATION:
Between 5 and 50000 compounds \are examined in the laboratory, of which only 100 to 200 are perfected in order to be tested on systems in vitro and in vivo.

Once the therapeutic target has been identified, scientists must then find one or more leads (e.g., chemical compounds or molecules) that interact with the therapeutic target so as to induce the desired therapeutic effects, e.g., through antiviral or antibacterial activity.

In order to discover the compounds whose pharmacological properties are likely to have the required therapeutic effects, researchers must test a large variety of them on one or more targets.

First of all, biologists ensure that the chosen compounds have the desired therapeutic or antiviral effects on the target. Then, they test the compounds relative toxicity or in the case of vaccine, their viral activity using in vitro cellular and/or tissue systems. Finally, they check their bioavailability in vivo on animals.

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