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Discovery of first-in-class therapeutics – venlafaxine (Effexor®), desvenlafaxine (Pristiq®), temsirolimus (Toresil®), ILS-920 and gemtuzumab ozogamicin (Mylotarg®)
The pharmaceutical industry today is experiencing unprecedented difficulty and faces enormous challenges, which include the industry’s declining efficiencies, patent expirations for key drugs, fierce price competition from generic drugs, mergers and acquisitions, high regulatory hurdles, declining innovation and the industry’s perceived tarnished image. Pharma has embarked on a range of initiatives to address these challenges, maintain its commitment to innovation and continue its mission to alleviate human suffering through the discovery of new medicines. This review covers the following themes: (1) drug discovery – highlighting process, targets, approach and current pharmaceutical platforms (small molecules, biologics and vaccines); (2) today’s realities – highlighting current challenges facing the pharmaceutical industry, especially the innovation gap, and Pharma’s commitment to innovation; (3) commitment to innovation and success stories focusing on selected examples of first-in-class therapeutics, such as the serotonin–noradrenaline reuptake inhibitor antidepressants venlafaxine (Effexor®, Pfizer, Surrey, UK) and desvenlafaxine (Pristiq®, Pfizer, Surrey, UK), immunophilin mammalian target of rapamycin modulator temsirolimus (Toresil®, Pfizer, Surrey, UK), the neuroprotectant ILS-920 for stroke therapy and the first conjugate anticancer drug gemtuzumab ozogamicin (Mylotarg®, Pfizer, Surrey, UK). Although many high drug discovery hurdles remain, the future holds great promise. The search continues for major breakthrough therapies that address unmet medical needs, such as disease-halting drugs for the treatment of Alzheimer’s disease, drugs to eradicate hepatitis C and acquired immune deficiency syndrome, and drugs to attack resistant cancers, treat strokes and alleviate cardiovascular disease.