Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C29H28F7NO2 |
| Molecular Weight | 555.5269 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](O[C@H]1CC[C@@H]2CN(C[C@H]2[C@@H]1C3=CC=C(F)C=C3)C4=CC(=O)CC4)C5=CC(=CC(=C5)C(F)(F)F)C(F)(F)F
InChI
InChIKey=FLNYCRJBCNNHRH-OIYLJQICSA-N
InChI=1S/C29H28F7NO2/c1-16(19-10-20(28(31,32)33)12-21(11-19)29(34,35)36)39-26-9-4-18-14-37(23-7-8-24(38)13-23)15-25(18)27(26)17-2-5-22(30)6-3-17/h2-3,5-6,10-13,16,18,25-27H,4,7-9,14-15H2,1H3/t16-,18-,25-,26+,27+/m1/s1
| Molecular Formula | C29H28F7NO2 |
| Molecular Weight | 555.5269 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Serlopitant, Originally developed by Merck, is a once-daily oral NK1 receptor antagonist being developed for the treatment of pruritus, or itch, associated with various conditions such as prurigo nodularis, psoriasis and chronic pruritus of unknown origin. It is highly selective for the human NK1 receptor and in both animal and human testing it has been well tolerated. In 2012, Merck licensed serlopitant to Menlo to develop it in indications other than nausea and vomiting. Development of serlopitant for the treatment of overactive bladder, alcohol dependence and pruritus was discontinued at phase II, by Merck & Co. and Japan. Menlo has completed three positive Phase 2 clinical trials with serlopitant showing a statistically significant reduction in pruritus compared to placebo. Serlopitant has been evaluated in over 1,600 patients and has been shown to be well-tolerated, including in patients who have received treatment for up to one year. Serlopitant is an investigational drug that is not currently approved for use in any indication in any country.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Serlopitant reduced pruritus in patients with prurigo nodularis in a phase 2, randomized, placebo-controlled trial. | 2019-05 |
|
| Serlopitant for the treatment of chronic pruritus: Results of a randomized, multicenter, placebo-controlled phase 2 clinical trial. | 2018-05 |
|
| A multicenter, double-blind, randomized, placebo controlled trial of a neurokinin-1 receptor antagonist for overactive bladder. | 2010-08 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30894279
In a randomized, double-blind, placebo-controlled study, 128 patients with chronic, treatment-refractory prurigo nodularis (PN) for more than 6 weeks received serlopitant, 5 mg, or placebo orally once daily for 8 weeks.
Route of Administration:
Oral
| Substance Class |
Chemical
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277V92K32B
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C267
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