Drug intelligence / Profile preview

trichosanthin

Development stage
Phase 2
Modality
Plant Toxin Conjugates → Immunotoxins → Antibody Conjugates → Antibody-Based Therapeutics, Recombinant Proteins and Enzymes, Bacterial Toxin Conjugates → Immunotoxins → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Intramuscular, Intra-amniotic, Intratumoral
01

Overview

Trichosanthin is a ribosome-inactivating protein (RIP) isolated from the root tuber of the Chinese medicinal herb Trichosanthes kirilowii Maxim. Traditionally used as an abortifacient in Chinese medicine (notably as part of Tian Hua Fen), it was later purified for clinical use to reduce side effects[1][2]. Trichosanthin acts as an rRNA N-glycosylase by hydrolyzing and depurinating adenylic acid at position 4324 in the α-sarcin/ricin loop on 28S rRNA of eukaryotic ribosomes, thereby inhibiting protein synthesis and leading to cell death[1][6][8]. It has demonstrated multiple pharmacological properties including immunomodulatory, anti-tumor (notably against gastric, colorectal, and non-small cell lung cancer), and antiviral activities—most notably blocking HIV replication and destroying HIV-infected macrophages[2][3][4][5]. Its mechanism also involves interaction with chemokine receptors such as CCR5 and CXCR4. Clinical studies have explored its use in HIV infection (Phase 2 trials) and various cancers; however, adverse reactions like immune responses and short plasma half-life have limited its broader application. Modifications such as immunotoxins or PEGylation have been investigated to improve its pharmacological profile[1].

Brand names
GLQ223GLQ-223GLQ 223
Other names
Tian Hua Fen
02

Targets

CXCR4 (C-X-C motif chemokine receptor 4)28S rRNA (28S ribosomal RNA)CCR5 (C-C chemokine receptor type 5)

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