Antibodies That Block Tumor Necrosis Factor Alpha (TNFα)

This 2000 patent describes specific human antibodies designed to strongly bind and neutralize a protein called TNFα, which is linked to inflammation and autoimmune diseases.

What it covers

This patent describes specific human antibodies, or parts of them, that are engineered to latch onto a molecule called human tumor necrosis factor alpha (hTNFα). The key is how well and how long they stick: they must bind very tightly (dissociating with a K d of 1x10^-8 M or less) and stay attached for a significant time (dissociating with a K off rate constant of 1x10^-3 s^-1 or less). These binding characteristics allow the antibodies to effectively block the harmful activity of hTNFα, as shown by their ability to neutralize hTNFα's toxicity in lab tests (IC 50 of 1x10^-7 M or less). The patent also details specific sequences for parts of these antibodies, like the CDR3 regions of their light and heavy chains, which are crucial for binding. These antibodies can be used to detect hTNFα or to treat conditions where hTNFα causes problems, such as inflammatory diseases.

What it doesn't cover

• —Antibodies that do not bind human TNFα.
• —Antibodies that bind human TNFα but do not meet the specific binding affinity (K d) or dissociation rate (K off) thresholds.
• —Antibodies that bind human TNFα but do not neutralize its cytotoxic activity in the specified L929 assay.
• —Antibodies that are not human or are not derived from human sequences.
• —Antibodies that bind to other molecules besides human TNFα.

The clever bit

The inventors precisely defined the required binding characteristics (affinity and dissociation rate) and neutralization potency for human antibodies against TNFα, specifying exact performance metrics and even particular amino acid sequences for critical binding regions.

Why it matters

Tumor Necrosis Factor alpha (TNFα) is a key protein involved in inflammation. When overactive, it contributes to diseases like rheumatoid arthritis, Crohn's disease, and psoriasis. This patent provided a foundational technology for developing highly effective biologic drugs that target and neutralize TNFα, significantly improving treatment options for millions suffering from autoimmune and inflammatory conditions.

Real-world examples

• 1.Biologic drugs for rheumatoid arthritis
• 2.Treatments for Crohn's disease
• 3.Therapies for psoriasis