Drug intelligence / Profile preview

Taphalgin

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules, Peptides
Administration
Subcutaneous
01

Overview

Taphalgin is a first-in-class tetrapeptide analgesic developed by PVP Labs, a Singapore-based biotechnology company. The drug's active ingredient is tyrosyl-D-arginyl-phenylalanyl-glycinamide acetate (H-Tyr-D-Arg-Phe-Gly-NH2), which is a synthetic derivative of the natural opioid peptide dermorphine. Taphalgin functions through a dual mechanism of action, acting as a μ1-selective opioid receptor agonist and a calcium channel modulator. It is designed to treat acute postoperative and cancer-related pain, offering a non-addictive alternative to traditional opioids like morphine without the associated risks of tolerance, respiratory depression, or addiction. Administered via subcutaneous injection, Taphalgin has completed multiple clinical trials with over 100,000 documented human exposures and is approved for use in markets outside the United States, while currently advancing toward U.S. clinical development.

Brand names
TAPHALGIN
Other names
tyrosyl-D-arginyl-phenylalanyl-glycinamide acetateH-Tyr-D-Arg-Phe-Gly-NH2H-Tyr-D-Arg-Phe-Gly-NH-2H-Tyr-D-Arg-Phe-Gly-NH 2Tafalgin
02

Targets

CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)MOR (Mu opioid receptor)CaV (Voltage-gated calcium channel protein complex)

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