Drug intelligence / Profile preview

tetrandrine

Development stage
Phase 4
Lead developer
Millenia Hope Pharmaceuticals
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous (as Injection)
01

Overview

Tetrandrine is a bis-benzylisoquinoline alkaloid extracted from the dried root of Stephania tetrandra S. Moore (commonly known as Han Fang Ji in traditional Chinese medicine)[4][5]. It has been used clinically for nearly 50 years in China to treat silicosis and is also indicated for rheumatoid arthritis and other autoimmune diseases[5][6][9]. Tetrandrine exhibits multiple pharmacological activities including anti-fibrotic, anti-inflammatory, immunosuppressive, antitumor (notably lung cancer), antiviral (including activity against Ebola virus and SARS-CoV-2), and radiosensitizing effects[2][5][7]. Mechanistically, it inhibits voltage-gated calcium channels and Ca2+-activated potassium channels[1], modulates protein kinase C signaling in T lymphocytes[6], suppresses proliferation of fibroblasts and immune cells such as B lymphocytes and macrophages[6], induces apoptosis in tumor cells by affecting pathways involving PARP, Bax, ICAM-1, VEGF/HIF-1α signaling[5], regulates P-glycoprotein-mediated drug resistance genes like MDR1 mRNA expression[2], blocks two-pore channel 2 (TPC2) to inhibit viral replication (SARS-CoV-2)[5], and acts as a radiosensitizer by promoting cell cycle progression from G2 to M phase after irradiation in cancer cells[2].

Brand names
CBT-1CBT1CBT 1
Other names
汉防己甲素Han Fang Ji Jia Su粉防己碱TET
02

Targets

ABCB1 (P-glycoprotein)KCNN1 (Small conductance calcium-activated potassium channel protein 1)PKC (Protein kinase C family)TPC2 (Two pore segment channel 2)CaV (Voltage-gated calcium channel protein complex)

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