Fundamentals of Medicinal Chemistry

(Brent) #1
The use of animals in drug testing is the subject of considerable debate in the

pharmaceutical industry as well as by the general public. Most countries are

committed to reducing the number of animals used in this way to a minimum

and are actively investigating the use of chemical and other alternative methods.

These methods include avoiding replication of experiments by different countries

centralizing their validation procedures, using human cellin vitrotests instead of

animalin vivotests and eliminiating methods that are not relevant to humans.

However, it is unlikely that it will be possible to replace all animal testing. Once

the drug has passed the preclinical trials it undergoes clinical trials in humans.

These trials can raise legal and ethical problems and so must be approved by the

appropriate legal and ethical committees before the trials are conducted. In most

countries this approval requires the issuing of a certificate or licence by the

appropriate medicine control agency (see section 11.8).

In order to accurately assess the results of a clinical trial, the results must be

compared with the normal situation and so, in the trials conducted on healthy

humans, 50%of the subjects are normally given an inactive substance in a form

that cannot be distinguished from the test substance. This inactive dosage form is

known as aplacebo. Furthermore, the results of a trial must be reliable and not

subject to influence by either the person conducting the trial or the recipient of

the drug. Consequently, it is now common practice to carry out adouble blind

procedure, where both the administrator of the drug and the recipient are

unaware whether they are dealing with the drug itself or a placebo. In addition,

subjects are randomly chosen to receive either the placebo or the drug.

Trials conducted on healthy subjects do not demonstrate the beneficial action

of the new drug. It is necessary to carry out double blind trials on unhealthy

patients to assess its efficacy. However, the use of a placebo with patients who

are ill raises moral and ethical considerations. Placebos may still be used if the

withdrawal of therapy causes no lasting harm to patients. If this is not possible,

the effect of the new drug is compared with that of an established drug used to

treat the medical condition. This reference drug should be carefully selected. It

should not be chosen so as to give the new drug an inflated degree of potency

that could be used to give the manufacturer an unfair commercial advantage

and the patient an inaccurate idea of the medicine’s effectiveness. A third

alternative is to usecross overtrials. Halfway through the trial the patients

receiving the drug are switched to either the placebo or the reference drug and

the patients receiving the placebo or reference drug are given the new drug. This

is ethically more acceptable as both groups have been exposed to the benefits of

the new drug.

The first clinical trials (Phase Itrials) are usually conducted on small groups

of healthy volunteers, which do not include children and the elderly. These

232 DRUG DEVELOPMENT AND PRODUCTION

Free download pdf