Over the years, a tendency toward biopharmaceutical products as therapeutics has been witnessed compared with small molecular drugs. Biopharmaceuticals possess greater specificity, selectivity and potency with fewer side effects. The pulmonary route is a potential noninvasive route studied for the delivery of various molecules, including biopharmaceuticals. It directly delivers drugs to the lungs in higher concentrations and provides greater bioavailability than other noninvasive routes. This review focuses on the pulmonary route for the delivery of biopharmaceuticals. We have covered various biopharmaceuticals, including peptides, recombinant proteins, enzymes, monoclonal antibodies and nucleic acids, administered via a pulmonary route and discussed their rewards and drawbacks.