palovarotene
Description
Palovarotene: a retinoic acid receptor gamma agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 10295295 |
CHEMBL ID | 2105648 |
CHEBI ID | 188559 |
SCHEMBL ID | 4658931 |
MeSH ID | M0542895 |
Synonyms (52)
Synonym |
---|
D09365 |
palovarotene (usan/inn) |
410528-02-8 |
CHEBI:188559 |
palovarotene |
4-[(e)-2-[5,5,8,8-tetramethyl-3-(pyrazol-1-ylmethyl)-6,7-dihydronaphthalen-2-yl]ethenyl]benzoic acid |
palovarotene [usan:inn] |
ipn60120 |
who 9025 |
benzoic acid, 4-((1e)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-(1h-pyrazol-1-ylmethyl)-2-naphthalenyl)ethenyl)- |
r 667 |
ro3300074 |
unii-28k6i5m16g |
rg-667 |
4-((1e)-2-(5,5,8,8-tetramethyl-3-(1h-pyrazol-1-ylmethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl)benzoic acid |
clm-001 |
28k6i5m16g , |
ro 3300074 |
r-667 |
ro-3300074 |
ipn-60120 |
CHEMBL2105648 |
palovarotene [usan] |
palovarotene [jan] |
4-{(1e)-2-[5,5,8,8-tetramethyl-3-(1h-pyrazol-1-ylmethyl)-5,6,7,8-tetrahydronaphthalen-2-yl]ethenyl}benzoic acid |
palovarotene [who-dd] |
palovarotene [inn] |
sohonos |
CS-2031 |
HY-14799 |
YTFHCXIPDIHOIA-DHZHZOJOSA-N |
4-[(e)-2-(5,5,8,8-tetramethyl-3-pyrazol-1-ylmethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)vinyl]benzoic acid |
SCHEMBL4658931 |
gtpl8276 |
r667 |
AKOS030526809 |
palovarotene(r 667) |
(e)-4-(2-(3-((1h-pyrazol-1-yl)methyl)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid |
DB12320 |
BCP16664 |
ZB1580 |
Q15708269 |
EX-A3101 |
A914214 |
MS-27181 |
DTXSID301025696 |
r 667;ro 3300074 |
palovaroteno |
4-((1e)-2-(5,5,8,8-tetramethyl-3-((1h-pyrazol-1-yl)methyl)-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl)benzoic acid |
palovarotenum |
clementia (proposed trade name) |
AC-36331 |
Research Excerpts
Overview
Palovarotene (Sohonos™) is an orally bioavailable selective retinoic acid receptor (RAR)γ agonist being developed by Ipsen for the reduction of heterotopic ossification (HO) formation in patients with fibrodysplasia ossificans progressiva (FOP) At 20 mg/day is a not a clinical inducer of CYP3A4.
Effects
Excerpt | Reference | Relevance |
---|---|---|
"Palovarotene has been shown to reduce bone formation in traumatic and genetic models of HO." | ( Palovarotene inhibits connective tissue progenitor cell proliferation in a rat model of combat-related heterotopic ossification. Boehm, CA; Bova, W; Cilwa, KE; Davis, TA; Dey, D; Forsberg, JA; Iwamoto, M; Muschler, GF; Potter, BK; Qureshi, AT; Sanders, EM; Seavey, JG; Tomasino, AM; Wheatley, BM, 2018) | 2.64 |
Treatment
Palovarotene treated animals exhibited significantly decreased expression of osteo- and chondrogenic genes by POD-7, including BMP4 (p = 0.02) pretreatment did not reduce FAPs' skeletogenic potential, indicating that efficacy requires chronic administration.
Toxicity
Excerpt | Reference | Relevance |
---|---|---|
" Overall, 89 treatment-emergent ocular adverse events (TEOAEs) were reported by 22 participants (61." | ( A Randomised Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of Palovarotene Ophthalmic Solution. Foster, WJ; Roach, JM; Small, KW; Strahs, AL, 2023) | 1.13 |
Pharmacokinetics
Japanese and non-Japanese groups had similar pharmacokinetic profiles. Palovarotene dose adjustments are not necessary for Japanese patients with FOP.
Compound-Compound Interactions
Excerpt | Reference | Relevance |
---|---|---|
" The trial also examined how palovarotene might interact with other treatments that are broken down by the body in the same way as palovarotene." | ( The Pharmacokinetic Profile of Palovarotene: An Open-Label Phase I Trial Investigating the Effect of Food and Potential for Drug-Drug Interaction in Healthy Participants. Dube, L; Le Quan Sang, KH; Marino, R; Ogier, J, 2023) | 1.49 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
"Palovarotene (Sohonos™) is an orally bioavailable selective retinoic acid receptor (RAR)γ agonist being developed by Ipsen for the reduction of heterotopic ossification (HO) formation in patients with fibrodysplasia ossificans progressiva (FOP)." | ( Palovarotene: First Approval. Hoy, SM, 2022) | 3.61 |
Dosage Studied
Palovarotene inhibited chondrogenic differentiation in vitro and reduced HO in juvenile FOP mice. Daily dosing resulted in aggressive synovial joint overgrowth and long bone growth plate ablation.
Drug Classes (1)
Class | Description |
---|---|
stilbenoid | Any olefinic compound characterised by a 1,2-diphenylethylene backbone. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Research
Studies (26)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (3.85) | 29.6817 |
2010's | 15 (57.69) | 24.3611 |
2020's | 10 (38.46) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 44.52
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (44.52) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 5 (19.23%) | 5.53% |
Reviews | 5 (19.23%) | 6.00% |
Case Studies | 1 (3.85%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 15 (57.69%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |