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The SARfaris: GPCR, Kinase, ADME

Thursday, 14 May 2009

New Drug Approvals - Pt. III - Golimumab (Simponi)

Third on our series of posts on new FDA drug approvals this year is Golimumab, approved on the 24th of April. Golimumab is a tumor necrosis factor alpha (TNFα) blocker indicated for the treatment of active forms of rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis. Golimumab is the fourth TNF inhibitor, after Etanercept, Infliximab and Adalimumab, to reach the market. Etanercept is a fusion protein of an engineered from the the TNF receptor fused to IgG1, while Infliximab and Adalimumab are very similar to Golimumab structurally in that they are all 'conventional' monoclonal antibodies. Golimumab (previously known as CNTO-148) is a human monoclonal antibody that exhibits multiple glycoforms with molecular weights of ca. 151 kDa. Golimumab has a good subcutaneous (sc) absorption (ca. 53% bioavailable), a plasma half-life of ca. 2 weeks, a volume of distribution of 58 to 126 mL/kg and a systemic clearance of 4.9 to 6.7 mL/day/kg. The recommended dosage of 50 mg is administrated by subcutaneous injection just once a month. The full prescribing information can be found here.

Golimumab has a boxed warning (colloquially known as a 'black box').

Golimumab is a monomeric immunoglobulin (IgG) consisting of four polypeptide chains in a "Y"- shaped form: two identical heavy chains of ~450 aminoacids and two identical light chains of ~217 animoacids, connected by disulfide bonds.

Golimumab molecular formula: C6530H10068N1752O2026S44

Golimumab CAS registry: 476181-74-5

The license holder for Golimumab is Centocor Ortho Biotech Inc. and the product website is

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