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hydroxytriptolide
- Development stage
- Phase 2
- Lead developer
- Allist Pharmaceuticals, Inc.
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Hydroxytriptolide (LLDT-8) is a synthetic derivative of triptolide, extracted from the Chinese medicinal plant Tripterygium wilfordii. It is a small molecule immunosuppressant and transcription inhibitor with lower cytotoxicity and higher immunosuppressive activity compared to its parent compound. Hydroxytriptolide has demonstrated potent anti-inflammatory effects by inhibiting proliferation and invasion of fibroblast-like synoviocytes in rheumatoid arthritis through modulation of the WAKMAR2/miR-4478/E2F1/p53 axis. It also acts as an inhibitor of inducible nitric oxide synthase (NOS2) and has shown broad-spectrum antitumor activity via general inhibition of gene transcription. In clinical studies, it has been investigated for enhancing CD4 T cell recovery in HIV-infected immunological non-responders on antiretroviral therapy and for treating rheumatoid arthritis[4][6][5]. The drug is currently in phase II clinical trials in China.
- Brand names
- LLDT-8LLDT8LLDT 8
- Other names
- (5R)-5-hydroxytriptolide
02
Targets
MIF–CD74 (Macrophage migration inhibitory factor–CD74 signaling pathway)NOS2 (Nitric Oxide Synthase 2)
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