2024-11-16-世界卫生组织-INN_Recommended_List_92_241页_3mb

Summary of International Nonproprietary Names for Pharmaceutical Substances (INN)

Core Content

The document provides a list of Recommended International Nonproprietary Names (INN) for pharmaceutical substances, specifically focusing on monoclonal antibodies. These names are standardized for global use in medicine and pharmacy, ensuring consistency and clarity in drug identification. It also includes detailed chemical names, molecular formulas, graphic formulas, and post-translational modification information for these substances.

Main Points

• INN Overview: The INN system is designed to provide standardized, non-proprietary names for pharmaceutical substances. These names are selected by the World Health Organization (WHO) following a specific procedure.
• No Usage Recommendation: The inclusion of a name in the INN list does not imply any recommendation for its use in medicine or pharmacy.
• Cumulative Lists: Lists of proposed and recommended INN names can be found in Cumulative List No. 17, 2017, available only on CD-ROM.
• Multilingual Support: The names are provided in Latin, English, French, and Spanish for international accessibility.
• Monoclonal Antibodies: The document focuses on several monoclonal antibodies, including abenacianinum, albipagrastimum alfa, aldastotugum, admilparantum, amostomigum, and amlenetugum, with detailed structural and functional information.

Key Information

1. abenacianinum / abenacianina

• INN: abenacianinum
• Chemical Description: A complex molecule with a detailed chemical structure.
• Molecular Formula: $C_{127}H_{145}CIF_4N_{10}O_{23}S_5$
• Post-translational Modifications:
  • Disulfide Bridges: Locations include intra-heavy chain and intra-light chain positions.
  • N-glycosylation Sites: H CH2 N84.4 at positions 297, 297".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present in the molecule.
  • C-terminal Lysine Clipping: H CHS K2 at position 449, 449".

2. albipagrastimum alfa

• INN: albipagrastimum alfa
• Chemical Description: Human serum albumin fused to human granulocyte colony-stimulating factor.
• Molecular Formula: Not explicitly provided.
• Post-translational Modifications:
  • Disulfide Bridges: Intra and inter positions are detailed.
  • N-glycosylation Sites: H VH 66 at 59, 59", H CH2 N84.4 at 299, 299".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present.
  • C-terminal Lysine Clipping: H CHS K2 at 449, 449".

3. aldastotugum

• INN: aldastotugum
• Chemical Description: Monoclonal antibody targeting SIGLEC15.
• Molecular Formula: Not explicitly provided.
• Post-translational Modifications:
  • Disulfide Bridges: Intra and inter positions.
  • N-glycosylation Sites: H CH2 N84.4 at 296, 296".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present.
  • C-terminal Lysine Clipping: H CHS K2 at 449, 449".

4. admilparantum

• INN: admilparantum
• Chemical Description: A monoclonal antibody targeting CXCL8.
• Molecular Formula: $C_{22}H_{31}N_5O_5$
• Post-translational Modifications:
  • Disulfide Bridges: Intra and inter positions.
  • N-glycosylation Sites: H VH 66 at 59, 59".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present.
  • C-terminal Lysine Clipping: H CHS K2 at 449, 449".

5. amlenetugum

• INN: amlenetugum
• Chemical Description: Monoclonal antibody targeting SNCA.
• Molecular Formula: Not explicitly provided.
• Post-translational Modifications:
  • Disulfide Bridges: Intra and inter positions.
  • N-glycosylation Sites: H CH2 N84.4 at 296, 296".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present.
  • C-terminal Lysine Clipping: H CHS K2 at 449, 449".

6. amostomigum

• INN: amostomigum
• Chemical Description: A bispecific monoclonal antibody targeting CD47 and CD274.
• Molecular Formula: Not explicitly provided.
• Post-translational Modifications:
  • Disulfide Bridges: Intra and inter positions.
  • N-glycosylation Sites: H VH 66 at 59, 59", H CH2 N84.4 at 296, 296".
  • Fucosylated Complex Bi-antennary CHO-type Glycans: Present.
  • C-terminal Lysine Clipping: H CHS K2 at 449, 449".
  • Produced in CHO-S Cells: Glycoform alfa.

General Post-translational Modifications

Disulfide Bridges Location

• Intra-H (Heavy Chain): 22-96, 143-199, 260-320, 366-424
• Intra-L (Light Chain): 23'-89', 135'-195'
• Inter-H-L (Heavy-Light Chain): 219-215', 219"-215"
• Inter-H-H (Heavy Chain): 225-225", 228-228"

Oxidation Sites

• M123, M298, M329, M548, W703, M711, M722

Deamidation Sites

• N18, Q29, Q32, Q33, N61

N-glycosylation Sites

• H CH2 N84.4: 296, 296" (for amlenetugum and aldastotugum)
• H VH 66: 59, 59" (for albipagrastimum alfa and admilparantum)

Glycoform

• All listed antibodies are in the glycoform alfa.

Conclusion

The document outlines the Recommended INN for various monoclonal antibodies, emphasizing the importance of standardized naming in pharmaceutical science. It also provides detailed structural and post-translational modification data, which are essential for understanding the molecular characteristics and production processes of these therapeutic agents. The information is available in multiple languages and is produced using CHO cells or Pichia pastoris, with a focus on glycosylation patterns and disulfide bridge locations.