mirogabalin: for the treatment of diabetic peripheral neuropathic pain
ID Source | ID |
---|---|
PubMed CID | 59509752 |
CHEMBL ID | 3545125 |
SCHEMBL ID | 1816421 |
MeSH ID | M000606774 |
Synonym |
---|
S6632 |
ds 5565 |
((1r,5s,6s)-6-(aminomethyl)-3-ethylbicyclo(3.2.0)hept-3-en-6-yl)acetic acid |
1138245-13-2 |
mirogabalin |
mirogabalin [inn] |
unii-s7lk2kdm5u |
mirogabalin [usan:inn] |
a 200-0700 |
s7lk2kdm5u , |
aminomethyl)-3-ethyl-bicyclo(3.2.0)hept-3-ene-6-acetic acid |
bicyclo(3.2.0)hept-3-ene-6-acetic acid, 6-(aminomethyl)-3-ethyl-, (1r,5s,6s)- |
a200-0700 |
[(1r,5s,6s)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid |
mirogabalin [who-dd] |
a-200-0700 |
mirogabalin [usan] |
SCHEMBL1816421 |
gtpl8303 |
2-[(1r,5s,6s)-6-(aminomethyl)-3-ethyl-6-bicyclo[3.2.0]hept-3-enyl]acetic acid |
AC-29882 |
CHEMBL3545125 |
2-((1r,5s,6s)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid |
AS-73453 |
2-[(1r,5s,6s)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid |
CS-6008 |
HY-12650 |
EX-A1736 |
bicyclo[3.2.0]hept-3-ene-6-acetic acid, 6-(aminomethyl)-3-ethyl-, (1r,5s,6s)- |
DB11825 |
AKOS032945006 |
BCP29010 |
[(1r,5s,6s)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid |
FTBQORVNHOIASH-CKYFFXLPSA-N |
D11203 |
mirogabalin (usan/inn) |
AMY11272 |
mirogabalin-besylate |
mirogabalin (ds-5565) |
BM166964 |
gtpl12597 |
[3h]mirogabalin |
DTXSID001032301 |
EN300-20087478 |
Mirogabalin is a novel gabapentinoid drug with a hydrophobic bicyclo substituent on the γ-aminobutyric acid moiety that targets the voltage-gated calcium channel subunit α. The drug demonstrated safety and efficacy in a multicenter, randomized, double-blind, placebo-controlled 14-week study in Asian patients with PHN.
Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the a2delta-1 subunit of voltage-gated calcium (Ca2+) channels.
Mirogabalin besylate has been approved in several countries to treat peripheral neuropathic pain.
Mirogabalin is a treatment option for patients with neuropathic pain. Data specifically for Chinese individuals are limited to a single-dose study.
mirogabalin was safe and well tolerated in healthy Chinese participants at single and multiple doses of up to 15 mg twice-daily. Compared with placebo, mirogbalin was significantly associated with more adverse events of dizziness, increased weight, peripheral oedema and somnolence.
Three phase 1 pharmacokinetic (PK)/pharmacodynamics (PD) studies were conducted in healthy men and women to further characterize the safety, tolerability, and PK/PD of mirogabalin administration with or without food. Four randomized, double-blind, placebo-controlled, 4-period drug-drug interaction studies were done in healthy subjects.
Excerpt | Reference | Relevance |
---|---|---|
"A population pharmacokinetic model was developed to describe plasma concentrations of mirogabalin and lactam metabolite, obtained following a single oral dose of 5 mg mirogabalin to subjects with varying degrees of renal function." | ( Population pharmacokinetic modeling and simulation for assessing renal impairment effect on the pharmacokinetics of mirogabalin. Merante, D; Miller, R; Truitt, K; Yin, OQ, 2016) | 0.87 |
"Four randomized, double-blind, placebo-controlled, 4-period drug-drug interaction studies were conducted in healthy subjects to evaluate the pharmacokinetic and pharmacodynamic (PD) interactions between mirogabalin and commonly used central nervous system depressants." | ( Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Mirogabalin When Coadministered With Lorazepam, Zolpidem, Tramadol, or Ethanol: Results From Drug-Drug Interaction Studies in Healthy Subjects. Currie, A; Dishy, V; Dow, J; He, L; Ishizuka, H; Jansen, M; Mendell, J; Merante, D; Zahir, H, 2018) | 0.91 |
"Three phase 1 pharmacokinetic (PK)/pharmacodynamics (PD) studies were conducted in healthy men and women to further characterize the safety, tolerability, and PK/PD of mirogabalin administration with or without food and to guide the dose selection and regimen for phase 2 and 3 clinical development." | ( Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects: Results from phase 1 studies. Brown, K; Dishy, V; He, L; Hsu, C; Mendell, J; Ohwada, S; Warren, V; Zahir, H, 2018) | 0.92 |
" We investigated the pharmacokinetic parameters and bioequivalence of the 2 formulations, including the maximum plasma concentration and the area under the plasma concentration-time curve up to the last quantifiable time." | ( Pharmacokinetics and Bioequivalence of Mirogabalin Orally Disintegrating Tablets and Conventional Tablets in Healthy Japanese Participants. Eto, T; Ishizuka, H; Shinohara, S; Suzuki, K; Toyama, K; Yoshiba, S; Yoshihara, K, 2023) | 1.18 |
Four randomized, double-blind, placebo-controlled, 4-period drug-drug interaction studies were conducted in healthy subjects to evaluate the pharmacokinetic and pharmacodynamic (PD) interactions between mirogabalin and commonly used depressants.
Excerpt | Reference | Relevance |
---|---|---|
"Four randomized, double-blind, placebo-controlled, 4-period drug-drug interaction studies were conducted in healthy subjects to evaluate the pharmacokinetic and pharmacodynamic (PD) interactions between mirogabalin and commonly used central nervous system depressants." | ( Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of Mirogabalin When Coadministered With Lorazepam, Zolpidem, Tramadol, or Ethanol: Results From Drug-Drug Interaction Studies in Healthy Subjects. Currie, A; Dishy, V; Dow, J; He, L; Ishizuka, H; Jansen, M; Mendell, J; Merante, D; Zahir, H, 2018) | 0.91 |
" Coadministration of mirogabalin and metformin is well tolerated in healthy subjects with no evidence of a drug-drug interaction." | ( Effect of coadministration of metformin with mirogabalin: Results from a phase 1, randomized, open-label, drug-drug interaction study
. Currie, A; Dow, J; He, L; Zahir, H; Zaidi, F, 2018) | 1.06 |
Excerpt | Reference | Relevance |
---|---|---|
" After single doses of mirogabalin (15 mg), the bioavailability was considered equivalent in the fed and fasted states, indicating that mirogabalin can be taken without food restrictions." | ( Tolerability, pharmacokinetics, and pharmacodynamics of mirogabalin in healthy subjects: Results from phase 1 studies. Brown, K; Dishy, V; He, L; Hsu, C; Mendell, J; Ohwada, S; Warren, V; Zahir, H, 2018) | 1.04 |
Study showed the safety and stable pain management of a long-term flexible dosing regimen of mirogabalin 10 or 15 mg twice daily for 52 weeks in patients with PHN. Of 172 patients who completed the study, 149 received the highest dosage (15 mg twicedaily)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 22 (40.00) | 24.3611 |
2020's | 33 (60.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (56.70) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 21 (36.21%) | 5.53% |
Reviews | 9 (15.52%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 28 (48.28%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |