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Some basic knowledge about histidine in biologics, amino acid excipients
Date: 2025-12-16Read: 0

Do you know what histidine is? What is the function of histidine? Which drugs have they been applied to again?


Histidine is a common amino acid excipient in biologics (antibodies, ADCs, vaccines, etc.), with ① pH buffering system; ② Antioxidant; ③ Freeze drying protection and other functions.

Histidine has been used as a pH buffer for protein preparations such as antibody drugs. Histidine can also stabilize proteins in a solid state through non covalent interactions, while histidine hydrochloride can prevent protein inactivation during freeze-drying. In addition, histidine is also an antioxidant that can eliminate hydroxyl radicals in solution. Currently, over 40% of the approved antibody drugs have histidine and histidine hydrochloride added to their formulations.


Application of histidine:
ENHERTU(DS-8201)

ingredient

fam-trastuzumab deruxtecan-nxki

L-histidine

L-histidine hydrochloride

Polysorbate 80

sucrose

Water for Injection

content

100 mg

4.45 mg

20.2 mg

1.5 mg

450 mg

5 mL


Opdualag(Relatlimab)

ingredient

nivolumab

relatlimab

L-histidine

L-histidine hydrochloride

Triamine pentaacetic acid

Tween 80

sucrose

Content (per mL)

12 mg

4 mg

1.1 mg

2.7 mg

0.008 mg

0.5 mg

85.6 mg


Imjudo(Tremelimumab, 联合 durvalumab)

ingredient

tremelimumab-actl

Disodium edetate

L-histidine

L-histidine hydrochloride

Tween 80

trehalose

Content (per mL)

20 mg

0.09 mg

0.68 mg

3.3 mg

0.2 mg

76 mg