Formulation

In Vitro Functional Testing Methods for Monoclonal Antibody Biosimilars

The pressure to contain rising healthcare costs — combined with the number of innovator biologic drugs coming off patent (30 licensed biological drugs by 2015) — offers huge opportunities for developers of biosimilar products. In 2011, the global market size of the biosimilars industry was around US$2.5 billion. Global demand for such products — and monoclonal antibody (MAb) biosimilars, specifically — is estimated to grow at 8–17% from 2012 to 2016 (1). The advent of biosimilars should bring more affordable…

Drug Products for Biological Medicines

The California Separation Science Society (CASSS) held a Chemistry, Manufacturing, and Controls (CMC) Strategy Forum on drug products for biological medicines in July 2012 in Bethesda, MD. Topics included novel delivery devices, challenging formulations, and combination products. This CMC Strategy Forum aimed to promote an understanding of how best to increase the speed and effectiveness of drug product and device development for both large and small companies. Participants focused on areas that improve the likelihood for regulatory success, reduce risk,…

High-Yield Production of PASylated Human Growth Hormone Using Secretory E. coli Technology

Since the 1985 approval of the first recombinant human growth hormone (hGH, such as Protropin/somatrem human growth hormone from Genentech, now Roche), the number of clinical indications for therapy with hGH has steadily increased (1). That led to a highly successful drug with more than US$3 billion sales in 2011 (2). Even so, hGH shares a common problem with most other first-generation protein therapeutics: a very short plasma half-life of just about two hours in humans. Because such biologics are…

Drug Products for Biological Medicines

Traditionally, the CaSSS CMC Strategy Forum meetings have provided a scientific focus on the development of biotech drug substances and their manufacture and characterization, leaving the development of drug product formulation and filling, understanding primary containers, and considering novel delivery systems somewhat out of scope. Over recent years, however, the importance of investing more science and technology into drug product development has become evident as different product types, higher protein concentrations, and doses and requirements for improved delivery of biological…

The Influence of Polymer Processing on Extractables and Leachables

Polymers provide a unique set of material properties, including toughness, chemical resistance, versatility, and low cost for both multiple-use and single-use bioprocessing systems. Polymer materials are manufactured as fittings and tubing for research and development (R&D) laboratories, as containers for bulk chemical and biological storage, as filters and separation technologies for downstream processing, and as containers and bottles for drug substance storage. These components and systems are helping drug companies improve their manufacturing flexibility, reduce their operating costs and capital…

Tunable Half-Life Technology

While a constantly developing market puts increasing pressure on pharmaceutical companies to provide advanced and personalized therapies, the industry is investing heavily in the development of targeted biologics. The aim is often to take new therapeutics through clinical trials and to market as quickly as possible and to develop more novel, tailored drugs. One common challenge for many biologics is their short plasma half-life. That often leads to reduced bioavailability, meaning that an administered drug will clear from a patient’s…

PEGylation of Biologics

In the 1970s, life-science researchers envisioned protein therapeutics as the ultimate targeted therapy. Companies could use them to address genetic deficiencies and cancer, among other disease classes, as well as to nudge the immune system for treating autoimmune disorders. The first therapeutic proteins were derived from animal or microbial cells, so patients launched immune responses to them that could curtail their activity and produce dangerous side effects. PEGylation was initially used to prevent immune responses with such drugs. PEG is…

Preformulation Development of a Recombinant Targeted Secretion Inhibitor

Our company carried out a preformulation study on a recombinant targeted secretion inhibitor (TSI) with contract research organization (CRO) Avacta Analytical. In this protein, the binding domain of botulinum toxin is replaced to broaden the toxin’s therapeutic potential and allow drug development to be targeted towards a specific disease. In our study, we took advantage of the high-throughput, microvolume protein analysis of Avacta’s Optim 1000 fluorescence and light-scattering instrument (which is distributed in the United States by Pall Corporation). It…

Understanding the Patient Journey

    The biopharmaceutical industry is abuzz with talk regarding a 2011 US Food and Drug Administration (FDA) guidance on human factors and the mitigation of user-based risk in the development of medical devices (1). As expected, his talk is often accompanied by a sense of anxiety. Device developers and the growing number of biomanufacturers developing combination drug–device products now need answers to usability questions they are hardly familiar with. Wrong answers may have direct (and troubling) implications from a…

Polysorbates, Immunogenicity, and the Totality of the Evidence

    Protein aggregation underlies many deleterious effects for biotherapeutics. Principal among those are loss of efficacy, induction of unwanted immunogenicity, altered pharmacokinetics, and reduced shelf life. Consequently, aggregation-preventing surfactants are essential components of many protein formulations. They facilitate the development, manufacture, and stability of dosage forms by helping formulators manage protein aggregation and reduce interactions with container and delivery device surfaces. Monoclonal antibodies (MAbs) present difficulties with respect to aggregation because they usually require relatively high doses for therapeutic…