2024-08-10-世界卫生组织-INN_Proposed_List_131_318页_10mb

Summary of the Document

Core Content

The document provides information on Proposed International Nonproprietary Names (INNs) for pharmaceutical substances, specifically List 131. These names are under consideration by the World Health Organization (WHO) as potential standardized names for new substances. The names are provided in Latin, English, French, and Spanish, along with chemical names, molecular formulas, and CAS registry numbers for each substance.

Main Points

• INN Purpose: INNs are used to identify pharmaceutical substances in a standardized, non-proprietary way. They help in avoiding confusion caused by brand names and promote the use of common names in scientific and medical contexts.

• Provisional Nature: The inclusion of a name in the Proposed INN list does not imply any recommendation for its use in medicine or pharmacy. It is merely a proposed name for consideration.

• Feedback Period: Comments or formal objections to the proposed names can be submitted to the WHO INN Programme within four months of the publication date. For List 131, the deadline is 11 December 2024.

• Publication Date: The list was published on 12 August 2024 in WHO Drug Information.

Key Information

Substance: abipapogenum suvaplasmidum

• Proposed INN (Latin, English, French, Spanish): abipapogene suvaplasmid / abipapogène suvaplasmide / abipapogén suvaplasmido
• Chemical Description: DNA plasmid encoding a mutation-inactivated human papillomavirus type 16 E6/E7 fusion protein linked to the human cytokine CCL3L1 via a dimerization module. It is conjugated to satetraxetan, a DOTA derivative, and radiolabeled with actinium-225.
• Use: Antineoplastic (anti-cancer) gene therapy.
• Molecular Formula: Not explicitly listed, but the CAS number is 2939766-18-2.
• Post-translational Modifications:
  • Disulfide bridges locations: Intra-H (C23-C104) 22-96, 144-200, 261-321, 374-432; Intra-L (C23-C104) 23-88, 134-194; Inter-H-L (h 5-CL 126) 220-218'; Inter-H-H (h 11, h 14) 226-226", 229-229".
  • N-terminal glutaminyl cyclization: Q > pyroglutamyl (pE, 5-oxoprolyl).
  • N-glycosylation sites: H CH2 N84.4.
  • Fucosylated complex bi-antennary CHO-type glycans.

Substance: adargiminasum

• Proposed INN (Latin, English, French, Spanish): adargeminase / adargimine / adargiminasa
• Chemical Description: A fusion protein derived from Streptococcus sp. G148 protein G and Mycoplasma arginini arginine deiminase (EC:3.5.3.6), expressed in Escherichia coli.
• Use: Antineoplastic.
• Molecular Formula: 2756760-23-1 (CAS number).
• Post-translational Modifications:
  • Disulfide bridges locations: Intra-H (C23-C104) 22-96, 151-207, 268-328, 374-432; Intra-L (C23-C104) 23-88, 134-194; Inter-H-L (h 5-CL 126) 227-214'; Inter-H-H (h 11, h 14) 233-233", 236-236".
  • N-terminal glutaminyl cyclization: Q > pyroglutamyl (pE, 5-oxoprolyl).
  • N-glycosylation sites: H CH2 N84.4.
  • Fucosylated complex bi-antennary CHO-type glycans.

Substance: alcestobartum

• Proposed INN (Latin, English, French, Spanish): alcestobart / alcestobart / alcestobart
• Chemical Description: A humanized monoclonal antibody targeting LAG3 (CD223), conjugated to satetraxetan and radiolabeled with actinium-225.
• Use: Immunostimulant, antineoplastic.
• Molecular Formula: 2888563-73-1 (CAS number).
• Post-translational Modifications:
  • Disulfide bridges locations: Intra-H (C23-C104) 22-96, 139-195, 253-313, 359-417; Intra-L (C23-C104) 23-88, 135-195; Inter-H-L (CH1 10-CL 126) 126-215"; Inter-H-H (h 8, h 11) 218-218", 221-221".
  • N-terminal glutaminyl cyclization: Q > pyroglutamyl (pE, 5-oxoprolyl).
  • N-glycosylation sites: VH N57, H CH2 N84.4, H CHS N439.
  • Fucosylated complex bi-antennary CHO-type glycans.

Substance: aleniglipronum

• Proposed INN (Latin, English, French, Spanish): aleniglipron / aléniglipron
• Chemical Description: A glucagon-like peptide 1 (GLP-1) receptor agonist with a specific molecular structure.
• Use: Antineoplastic.
• Molecular Formula: Not explicitly listed, but the CAS number is 2911580-96-4.
• Post-translational Modifications:
  • Disulfide bridges locations: Intra-H (C23-C104) 22-96, 139-195, 253-313, 359-417; Intra-L (C23-C104) 23-88, 135-195; Inter-H-L (h 5-CL 126) 126-215"; Inter-H-H (h 8, h 11) 218-218", 221-221".
  • N-terminal glutaminyl cyclization: Q > pyroglutamyl (pE, 5-oxoprolyl).
  • N-glycosylation sites: VH N57, H CH2 N84.4, H CHS N439.
  • Fucosylated complex bi-antennary CHO-type glycans.

Additional Notes

• Post-translational Modifications: These include disulfide bridges, N-terminal glutaminyl cyclization, and N-glycosylation.
• Production: These substances are produced in Chinese hamster ovary (CHO) cells or Escherichia coli.
• Glycoforms: The substances are described as having glycoform alpha.
• No Glycans: Some substances have no glycans, while others have fucosylated complex bi-antennary CHO-type glycans.
• Peptide Linker: A specific peptide linker (48SGSNNNNNNGSGG60) is used in the adargiminasum substance.
• No Post-translational Modifications: For some substances, it is noted that no post-translational modifications are present.

Summary Table

Key Features of INN

• International Standardization: INNs are used globally to identify pharmaceutical substances.
• Non-proprietary: They are not trademarked and are intended for use in scientific and medical contexts.
• Provisional: The names are not finalized and may be subject to change.
• Feedback Mechanism: The WHO allows for public comments or objections within a four-month period.
• Scientific Basis: The proposed names are based on information from manufacturers and are not endorsed by WHO for efficacy or use.