| Stereochemistry | ACHIRAL |
| Molecular Formula | C25H20N4O.C4H6O4 |
| Molecular Weight | 510.5405 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CCC(O)=O.CN1C=C(C(=N1)C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C5=CC=NC=C5
InChI
InChIKey=AVSAEIJRBBJXNR-UHFFFAOYSA-N
InChI=1S/C25H20N4O.C4H6O4/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21;5-3(6)1-2-4(7)8/h2-16H,17H2,1H3;1-2H2,(H,5,6)(H,7,8)
| Molecular Formula | C4H6O4 |
| Molecular Weight | 118.088 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C25H20N4O |
| Molecular Weight | 392.4525 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
PF-2545920 is an orally-active phosphodiesterase 10A (PDE10A) inhibitor originated by Pfizer, for the treatment of Huntington's disease. PF-2545920 was originally developed by Pfizer for the treatment of schizophrenia. But later clinical studies for Schizophrenia were discontinued. PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.
CNS Activity
Originator
Approval Year
Cmax
Sourcing
| Vendor/Aggregator | ID | URL |
|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. | 2009 Nov |
Sample Use Guides
20 mg twice a day (BID) for 26 weeks. Each 20 mg dose will be taken as 4 tablets of 5 mg. The 20mg dose will be titrated as follow: 5mg BID for 7 days, 10mg BID for 7 days, 15 mg BID for 7 days and 20 mg BID to week 26. Study drug will be provided in weekly blister cards.
5 mg twice a day (BID) for 26 weeks. Each 5 mg dose will be taken as 4 tablets: one tablet of 5 mg and 3 tablets of matching placebo. The 5mg dose will not be titrated. Study drug will be provided in weekly blister cards.
Route of Administration:
Oral
Pf-2545920 comparably inhibited the growth of
all human colon cancer cell lines with IC 50 values ranging from 6.9 uM to 19.6 uM. Treatment of HT-29 cells with 10 uM Pf-2545920 increased the percentage of cells undergoing apoptosis
to 25.9% showing positive staining for Annexin V and
31.9% for both Annexin V and PI. Treatment of HT-29 cells with 25 uM Pf-2545920 further increased the percentage of
cells undergoing apoptosis with 38.2% showing positive
staining for Annexin V and 31.4 % for both Annexin V
and PI.
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
FDA ORPHAN DRUG | 429914 |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
100000183836 | PRIMARY | |||
|
1037309-45-7 | PRIMARY | |||
|
TJ5KAZ8T5G | PRIMARY | |||
|
24857794 | PRIMARY | |||
|
DTXSID90647726 | PRIMARY | |||
|
EU/3/16/1691(POSITIVE) | PRIMARY | On 14 July 2016, orphan designation (EU/3/16/1691) was granted by the European Commission to Pfizer Limited, United Kingdom, for 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline succinic acid for the treatment of Huntington's disease. |
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PARENT -> SALT/SOLVATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |