Cyclosporin, a novel drug, exhibiting unique discriminatory action on
the activation of helper lymphocytes without the undesirable side effe
cts associated with conventional immunosuppressants, can well be consi
dered as the prototype of a new generation of immunosuppressants. It i
s probably the first one to demonstrate that an immunopharmacologic ap
proach to the modulation of the immune response by drugs is feasible.
This enabled a decisive step forward to be made in transplantation sur
gery, particularly in the field of heart and kindney transplantation.
Cyclosporin A exerts antifungal, antiparasitic and antiinflammatory ac
tivities also. There is considerable interest in the prospective value
of this drug in the treatment of autoimmune disorders. Accolades are
to be given for its role as a tool for studying mechanisms of the immu
ne system. This review is an attempt to look into the various strides
it had evolved before attaining the status of a unique drug, and also
to assess critically the prospective value of this potent drug. The pr
esent modem era of antibiotic research is characterized by advanced sc
reening procedures aiming specifically not only at antibacterials or a
ntifungals but at compounds like enzyme inhibitors, immunomodulators a
nd antitumor drugs. New sources of rare microorganisms are currently u
nder exploitation. Development of microbial products with new medicina
l activties has turned out to be a big research area, spearheaded by t
he success story of small molecular weight immunomodulators. Long acce
pted as the best way to prevent or treat rejection in patients undergo
ing organ transplantation, immunosuppressive therapy is attracting inc
reased attention for its ability to treat a variety of diseases. One s
uch potent agent, widely acclaimed as the first of a new generation of
remarkable immunosuppressive agents, cyclosporin is being used in nov
el ways in a wide array of conditions. The cyclosporins are a group of
over 25 closely related cyclic undecapeptides produced as secondary m
etabolites by two strains of fungi imperfecti, Cylindrocarpum lucidum
BOOTH and Tolypocladium inflatum GAMS, isolated from soil samples. Cyc
losporin A is the main component of this family of cyclic peptides eac
h containing 11 amino acids. This review is a survey of the works of a
large team of chemists, biologists, clinicians, toxicologists and pha
rmacologists which lead to the development of a new drug of choice and
the impact that this drug in particular is having and hopefully other
similar ones will have in the field of immunopharmacology.