PF-06372865

a subtype-selective gamma-aminobutyric acid A (GABAA)-positive allosteric modulator lacking in functional activity at alpha 1-containing receptors

Also Known As:

7-ethyl-4-(3-(4-ethylsulfonyl-2-methoxyphenyl)-4-fluorophenyl)imidazo(4,5-c)pyridazine

Networked: 5 relevant articles (0 outcomes, 3 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Imidazoles: 150
      - PF-06372865: 5
  - Pyridazines: 11
    - PF-06372865: 5

Experts

1.	Gurrell, Rachel: 4 articles (08/2019 - 09/2018)
2.	Whitlock, Mark: 4 articles (08/2019 - 09/2018)
3.	Butt, Richard P: 3 articles (08/2019 - 09/2018)
4.	Dua, Pinky: 3 articles (08/2019 - 09/2018)
5.	Gorman, Donal: 2 articles (08/2019 - 01/2019)
6.	Reynolds, David S: 2 articles (01/2019 - 09/2018)
7.	Groeneveld, Geert Jan: 1 article (08/2019)
8.	Hay, Justin L: 1 article (08/2019)
9.	Okkerse, Pieter: 1 article (08/2019)
10.	Siebenga, Pieter S: 1 article (08/2019)

Related Diseases

1.	Seizures (Absence Seizure) 01/01/2019 - "Further study of the antiepileptic properties of PF-06372865 is warranted in patients with absence seizures." 01/01/2019 - "The aim of this study was to assess the antiepileptic effect of PF-06372865 in a preclinical model of absence seizures. "
2.	Epilepsy (Aura) 01/01/2019 - "The objective of this phase 2a study was to assess the activity of PF-06372865, a positive allosteric modulator (PAM) of α2/3/5 subunit-containing GABAA receptors with minimal activity at α1-containing receptors, which are believed to mediate many of the adverse events associated with benzodiazepines, in the epilepsy photosensitivity model as a proof-of-principle of efficacy. "
3.	Anxiety Disorders (Anxiety Disorder) 01/01/2019 - "An 8-Week, Randomized, Phase 2, Double-Blind, Sequential Parallel-Group Comparison Study of Two Dose Levels of the GABAA Positive Allosteric Modulator PF-06372865 Compared With Placebo as an Adjunctive Treatment in Outpatients With Inadequate Response to Standard of Care for Generalized Anxiety Disorder."
4.	Low Back Pain (Lumbago) 09/01/2018 - "At this time, a total of 222 patients were randomised and the mean PF-06372865 4-week response on the low back pain intensity was 0.16 units higher (worse) than placebo (90% confidence interval -0.28 to 0.60). " 09/01/2018 - "A randomised, placebo-controlled clinical trial with the α2/3/5 subunit selective GABAA positive allosteric modulator PF-06372865 in patients with chronic low back pain." 09/01/2018 - "The effect of PF-06372865, a subtype-selective positive allosteric modulator of the γ-aminobutyric acid type A (GABAA) receptor, on chronic low back pain was investigated in a randomised, placebo- and active-controlled phase 2 clinical trial. "
5.	Pain (Aches) 08/01/2019 - "A dose of 65 mg PF-06372865 led to an increase in PTT for the cold pressor at a ratio of 1.17 (90% CI: 1.03, 1.32), and pressure pain task: 1.11 (90% CI: 1.01, 1.21). " 08/01/2019 - "A dose of 15 mg PF-06372865 increased pain tolerance thresholds (PTTs) for pressure pain at a ratio of 1.11 (90% confidence interval [CI]: 1.02, 1.22) compared with placebo. "

Related Drugs and Biologics

1.	Benzodiazepines
2.	Anticonvulsants (Antiepileptic Drugs)
3.	Valproic Acid (Depakote)
4.	Diazepam (Valium)
5.	Aminobutyrates (Aminobutyric Acid)

Related Therapies and Procedures

1.	Electrodes (Electrode)