Formulation strategies in immunotherapeutic pharmaceutical products

Table 1 List of antibody products approved by the United States Food and Drug Administration in 2018 and through May 2019. Information source: www.fda.gov and each product’s package insert

Trade name	API	Yr	Sponsor	Excipients1	Form	Storage condition
Skyrizi	Risankizumab-rzaa	2019	Abbvie	Disodium succinate hexahydrate, polysorbate 20, sorbitol, and succinic acid	Liquid	2-8 °C, avoid light/shake/freeze
Evenity	Romosozumab-aqqg	2019	Amgen	Acetate, calcium, polysorbate 20, and sucrose	Liquid	2-8 °C, avoid light/shake/freeze
Cablivi	Caplacizumab-yhdp	2019	Ablynx/Ablynx	Citrate dihydrate, polysorbate-80, sucrose, and trisodium citrate dihydrate	Lyophilized Powder	2-8 °C, avoid light /freeze
Trogarzo	Ibalizumab-uiyk	2018	TaiMed Biologics/ Theratechnologies	L-histidine, polysorbate 80, sodium chloride, sucrose	Liquid	2-8 °C, avoid light/shake/freeze
Ilumya	Tildrakizumab	2018	Sun pharma	L-histidine, L-histidine hydrochloride monohydrate, polysorbate 80, sucrose	Liquid	2-8 °C, avoid light/shake/freeze
Crysvita	Burosumab-twza	2018	Ultragenyx pharmaceutical/kyowa hakko kirin	L-histidine, L-methionine, polysorbate 80, D-sorbitol	Liquid	2-8 °C, avoid light/shake/freeze
Aimovig	Erenumab-aooe	2018	AmgenNovartis	Acetate, polysorbate 80, sucrose	Liquid	2-8 °C, avoid light/shake/freeze
Poteligeo	Mogamulizumab-kpkc	2018	Kyowa hakko kirin	Citric acid monohydrate, glycine, polysorbate 80	Liquid	2-8 °C, avoid light/shake/freeze
Takhzyro	Lanadelumab	2018	Dyax/ Shire	Citric acid monohydrate, L-histidine, sodium chloride, sodium phosphate dibasic dihydrate	Liquid	2-8 °C, avoid light/shake/freeze
Lumoxiti	Moxetumomab pasudotox-tdfk	2018	AstraZeneca	Glycine, polysorbate 80, sodium phosphate monobasic monohydrate, sucrose	Lyophilized Powder	2-8 °C, avoid light/shake/freeze
Ajovy	Fremanezumab-vfrm	2018	Teva	Disodium ethylenediaminetetraacetic acid dihydrate (EDTA), L-histidine, L-histidine hydrochloride monohydrate, polysorbate-80, sucrose	Liquid	2-8 °C, avoid light/shake/freeze
Emgality	Galcanezumab-gnlm	2018	Eli Lilly	L-histidine, L-histidine hydrochloride monohydrate, polysorbate 80, sodium chloride	Liquid	2-8 °C, avoid light/shake/freeze
Libtayo	Cemiplimab-rwlc	2018	Regeneron/Sanofi	L-histidine, L-histidine monohydrochloride monohydrate, sucrose, L-proline, polysorbate 80	Liquid	2-8 °C, avoid light/shake/freeze

¹Water for injection and pH adjusting reagents, such as hydrochloric acid and/or sodium/potassium hydroxide, are not specified here. API: Active pharmaceutical ingredient.

Table 2 Non-amino acid buffer systems frequently used in antibody parenteral products

Buffer system	Controlled pH range (25 °C)	Acid	Base	Example product
Phosphate	5.8-7.8	Monosodium phosphate	Disodium phosphate	Tysabri®
Acetate	3.8-5.8	Acetic acid	Sodium acetate	Amgevita®
Citrate	3.0-7.4	Citric acid	Sodium citrate	Humira®
Succinate	3.3-6.6	Succinic acid	Sodium succinate	Kadcyla®
Tris	7-9	Tris-HCl	Tris	Besponsa®