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. Author manuscript; available in PMC: 2019 Apr 1.
Published in final edited form as: Nat Rev Drug Discov. 2018 Jan 5;17(4):243–260. doi: 10.1038/nrd.2017.229

Table 2.

Selected biased agonists under different phases of evaluation for therapeutic use.

Ligand Receptor Signalling bias Indication Development status
Carvedilol Beta 1 AR
Beta 2 AR
Mild βarrestin Congestive heart failure Approved
Oliceridine (TRV130) Mu opioid G protein Moderate to severe pain Phase III
TRV734 Mu opioid G protein Moderate to severe pain Phase I
Triazole 1.1 Kappa opioid G protein Pruritus Preclinical
RB-64 Kappa opioid G protein Pain Preclinical
PZM21 Mu opioid G protein Pain Preclinical
UNC9994, UNC9975 Dopamine 2 βarrestin Schizophrenia and mood disorders Preclinical
TRV250 Delta opioid G protein Migraine Preclinical