In the past few decades, antibody drugs have thoroughly revolutionized the pharmaceutical industry and saved countless lives. Since the introduction of the first approved monoclonal antibody drug, Orthoclone, in 1986, over 125 kinds of antibody drugs have been brought to market and achieved great success.
From 1986 to February 2021, a total of 126 antibody drugs have been approved for market, including 10 Antibody-Drug Conjugates (ADCs), 16 biosimilars, and 3 antibody fragments.
Among these 126 antibody drugs, 36 are lyophilized powders, and the rest are solutions. Their routes of administration are primarily subcutaneous injection or intravenous injection. Subcutaneous injection drugs are generally ready-to-use solutions or reconstituted lyophilized powders, requiring no dilution. In contrast, intravenous drugs are usually concentrated solutions for injection, which need to be diluted with saline or other intravenous fluids before administration. Most of these antibody drugs are available in single-dose forms, but there are exceptions, with some being packaged in vials, prefilled auto-injectors, or prefilled syringes.
The classic composition of antibody drug formulations includes antibodies, excipients for regulating solution osmolality or lyoprotectants for lyophilized powders, buffers, and surfactants. The ionic strength-regulating excipients mainly consist of sodium chloride and non-ionic strength regulators such as sucrose, trehalose, mannitol, maltose, and sorbitol. Lyoprotectants include trehalose and sucrose. The pH range of antibody drug solutions is between 4.0 and 8.0, with pH regulators including histidine, citric acid, succinic acid, acetic acid, phosphates, glutamic acid, adipic acid, aspartic acid, lactic acid, tromethamine, and 2-(N-morpholino)ethanesulfonic acid.
The surfactants are mainly polysorbate 20 or polysorbate 80. Four of these antibody drugs use poloxamer 188 as a surfactant.
Viscosity-reducing agents include sodium chloride, arginine, glycine, proline, and lysine. Arginine can also be used to adjust ionic strength and reduce antibody protein aggregation. Other excipients include antioxidants (methionine) and chelating agents (EDTA or DTPA).
The maximum dose for subcutaneous injection products among antibody drugs is 15 mL, which is usually required to be administered within 3-5 minutes. However, the typical injection dose is 0.5-2 mL. Some antibody drugs use hyaluronidase to enable large-volume subcutaneous injections (5-15 mL).
Updated: Dec 26, 2024
