Darigabat

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Darigabat
Clinical data
Other namesCVL-865; PF-06372865; PF-6372865
Routes of
administration
Oral administration
Drug classGABAA receptor positive allosteric modulator
Pharmacokinetic data
MetabolismCYP3A4[1]
Elimination half-life11 hours[1]
Identifiers
  • 7-ethyl-4-[3-(4-ethylsulfonyl-2-methoxyphenyl)-4-fluorophenyl]imidazo[4,5-c]pyridazine
JSmol)
  • CCN1C=NC2=C1N=NC=C2C3=CC(=C(C=C3)F)C4=C(C=C(C=C4)S(=O)(=O)CC)OC
  • InChI=1S/C22H21FN4O3S/c1-4-27-13-24-21-18(12-25-26-22(21)27)14-6-9-19(23)17(10-14)16-8-7-15(11-20(16)30-3)31(28,29)5-2/h6-13H,4-5H2,1-3H3
  • Key:PTTQXDBPTFOCMT-UHFFFAOYSA-N

Darigabat (developmental code names CVL-865, PF-06372865, PF-6372865) is a

chronic lower back pain, but development for these indications was discontinued.[2][3][4] It is taken via oral administration.[2]

Darigabat acts as a

elimination half-life of darigabat is 11 hours and it is metabolized mainly by CYP3A4.[1]

In clinical trials conducted thus far,

memory impairment, mild cognitive impairment, balance impairment, and feeling abnormal.[3][6] It has been described as well-tolerated.[3][4]

Darigabat was originated by Pfizer and is under development by Cerevel Therapeutics and Pfizer.[2] As of January 2023, it is in phase 2 clinical trials for epilepsy and seizures, phase 1 trials for panic disorder, and preclinical development for anxiety disorders.[2][3] Development for back pain was discontinued due to lack of effectiveness in a phase 2 trial, while development for generalized anxiety disorder was discontinued due to business reasons as well as lack of effectiveness in a phase 2 trial.[3][4][2]

See also

References

External links