Derfus Gayle E, Dizon-Maspat Jemelle, Broddrick Jared T, Velayo Arleene C, Toschi Josh D, Santuray Rodell T, Hsu Stephen K, Winter Charles M, Krishnan Rajesh, Amanullah Ashraf
Biologics Development; Gilead Sciences; Oceanside, CA USA.
MAbs. 2014 May-Jun;6(3):679-88. doi: 10.4161/mabs.28257. Epub 2014 Feb 19.
While many antibody therapeutics are formulated at low concentration (~10-20 mg/mL) for intravenous administration, high concentration (> 100 mg/mL) formulations may be required for subcutaneous delivery in certain clinical indications. For such high concentration formulations, product color is more apparent due to the higher molecular density across a given path-length. Color is therefore a product quality attribute that must be well-understood and controlled, to demonstrate process consistency and enable clinical trial blinding. Upon concentration of an IgG4 product at the 2000 L manufacturing scale, variability in product color, ranging from yellow to red, was observed. A small-scale experimental model was developed to assess the effect of processing conditions (medium composition and harvest conditions) on final bulk drug substance (BDS) color. The model was used to demonstrate that, for two distinct IgG4 products, red coloration occurred only in the presence of disulfide reduction-mediated antibody dissociation. The red color-causing component was identified as vitamin B 12, in the hydroxocobalamin form, and the extent of red color was correlated with the cobalt (vitamin B 12) concentration in the final pools. The intensity of redness in the final BDS was modulated by changing the concentration of vitamin B 12 in the cell culture media.
虽然许多抗体疗法制剂的静脉给药浓度较低(约10 - 20 mg/mL),但在某些临床适应症中,皮下给药可能需要高浓度(> 100 mg/mL)的制剂。对于此类高浓度制剂,由于在给定路径长度上分子密度较高,产品颜色更加明显。因此,颜色是一种产品质量属性,必须充分理解和控制,以证明工艺的一致性并实现临床试验的盲法操作。在2000 L生产规模下浓缩IgG4产品时,观察到产品颜色存在从黄色到红色的变化。开发了一个小规模实验模型来评估加工条件(培养基组成和收获条件)对最终原料药(BDS)颜色的影响。该模型用于证明,对于两种不同的IgG4产品,只有在存在二硫键还原介导的抗体解离时才会出现红色。导致红色的成分被鉴定为羟钴胺形式的维生素B12,并且红色程度与最终池中的钴(维生素B12)浓度相关。通过改变细胞培养基中维生素B12的浓度来调节最终BDS中的红色强度。