Page last updated: 2024-11-13

mna 715

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-2-hepten-6-ynamide: structure in first source; a derivative of A77 1726, the active metabolite of the antirheumatic drug leflunomide, where the isoxazole ring has opened to become a nitrile and an alkyne [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54686843
CHEMBL ID4754445
MeSH IDM0269242

Synonyms (31)

Synonym
manitimus
fk-778
hmr-1715
x-920715
mna-715
fk 778
malononitrilamide 715
2-cyano-3-hydroxy-n-(4-(trifluoromethyl)phenyl)-2-hepten-6-ynamide
mna 715
x 920715
mna-x 920715
185915-33-7
malononitrilamide-715
2-hepten-6-ynamide, 2-cyano-3-hydroxy-n-(4-(trifluoromethyl)phenyl)-, (z)-
2-cyano-3-hydroxy-n-(4-(trifluoromethyl)phenyl)-2-hepten-6-ynoic acid
unii-4b135rk2kl
4b135rk2kl ,
(2z)-2-cyano-3-hydroxy-n-(4-(trifluoromethyl)phenyl)hept-2-en-6-ynamide
2-hepten-6-ynamide, 2-cyano-3-hydroxy-n-(4-(trifluoromethyl)phenyl)-
manitimus [inn]
202057-76-9
hmr1715
(2z)-2-cyano-3-hydroxy-n-(4-(trifluoromethly)phenyl)-2-hepten-6-ynamide
hmr-1715 [who-dd]
DB06481
Q27259358
(z)-2-cyano-3-hydroxy-n-[4-(trifluoromethyl)phenyl]hept-2-en-6-ynamide
BM162377
irelroqhiplasx-seyxrhqnsa-n
CHEMBL4754445
AKOS040733665

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" A safe and effective immunosuppressive agent that does not predispose to viral infection is needed in transplantation."( Assessment of efficacy and safety of FK778 in comparison with standard care in renal transplant recipients with untreated BK nephropathy.
First, MR; Fitzsimmons, W; Guasch, A; Holman, J; Roy-Chaudhury, P; Woodle, ES, 2010
)
0.36
" Although the treatment with FK778 decreased BK viral load in this study, it was associated with a less favorable rejection profile and renal function and a higher incidence of serious adverse events compared with reduction of immunosuppression."( Assessment of efficacy and safety of FK778 in comparison with standard care in renal transplant recipients with untreated BK nephropathy.
First, MR; Fitzsimmons, W; Guasch, A; Holman, J; Roy-Chaudhury, P; Woodle, ES, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
"In a double-blind manner, 149 patients were randomized to a 12-week treatment with FK778 in combination with tacrolimus (Tac) and corticosteroids (S)."( The effects of FK778 in combination with tacrolimus and steroids: a phase II multicenter study in renal transplant patients.
Chang, R; Charpentier, B; Grinyó, JM; Jurewicz, A; Klinger, M; Kreis, H; Mourad, G; Neuhaus, P; Paczek, L; Paul, LC; Rostaing, L; Short, C; Squifflet, JP; van Hooff, JP; Vanrenterghem, Y; Wlodarczyk, Z, 2004
)
0.32
"We evaluated the in vitro capacity of FK778, alone or in combination with other immunosuppressive drugs: Tacrolimus (TRL); Sirolimus (SRL), Everolimus (EVL), to inhibit clonal expansion of T-lymphocytes and expression of lymphocyte-activation surface antigens; secondly, we compared the immunosuppressive potential of FK778 combined with TRL, SRL and EVL with the same combinations using Mycophenolic acid (MPA) as antimetabolite."( Role of FK778 alone or in combination with tacrolimus or mTOR inhibitors as an immunomodulator of immunofunctions: in vitro evaluation of T cell proliferation and the expression of lymphocyte surface antigens.
Barceló, JJ; Brunet, M; Fortuna, V; Jiménez, O; Millán, O,
)
0.13

Dosage Studied

ExcerptRelevanceReference
" At doses lower than 10 mg/kg daily, FK778 is cleared from the circulation between the dosing intervals, thus failing to exert its inhibitory effects on immune functions."( In vivo pharmacokinetic and pharmacodynamic evaluation of the malononitrilamide FK778 in non-human primates.
Bîrsan, T; Dambrin, C; Fitzsimmons, WE; Klupp, J; Larson, MJ; Morris, RE; Stalder, M, 2003
)
0.32
" Research and development programs are underway for a new modified release dosage form of tacrolimus (MR-4), a new analog of leflunomide (FK 778), and several novel compounds (PG 490-88, AGI 1096) in collaboration with other companies."( New drugs to improve transplant outcomes.
First, MR; Fitzsimmons, WE, 2004
)
0.32
" To fully benefit from this promising new drug, FK778 dosing will be optimized in subsequent studies."( The effects of FK778 in combination with tacrolimus and steroids: a phase II multicenter study in renal transplant patients.
Chang, R; Charpentier, B; Grinyó, JM; Jurewicz, A; Klinger, M; Kreis, H; Mourad, G; Neuhaus, P; Paczek, L; Paul, LC; Rostaing, L; Short, C; Squifflet, JP; van Hooff, JP; Vanrenterghem, Y; Wlodarczyk, Z, 2004
)
0.32
" The optimal FK778 dosage was determined to be 20 mg/kg per day, because adverse effects (weight loss and intestinal bleeding) occurred at 30 mg/kg per day."( FK778 and FK506 combination therapy to control acute rejection after rat liver allotransplantation.
Hirohashi, K; Ikeda, K; Kubo, S; Minamiyama, Y; Okuda, T; Suehiro, S; Takemura, S; Tanaka, H; Yamamoto, S; Yamasaki, K, 2004
)
0.32
"05) or 1 day after angioplasty in both dosage groups (group 1b, P<."( 2005 Dr. Gary J. Becker Young Investigator Award: periprocedural oral administration of the leflunomide analogue FK778 inhibits neointima formation in a double-injury rat model of restenosis.
Bolte, H; Brossmann, J; Fändrich, F; Hedderich, J; Heller, M; Jahnke, T; Müller-Hülsbeck, S; Rector, L; Schäfer, FK; Schäfer, PJ, 2005
)
0.33
" In addition, FK778 also reduced the levels of preformed circulating autoantibodies in adult mice, although the dosage required was 4 times higher than that used in neonates."( Leflunomide derivative FK778 inhibits production of antibodies in an experimental model of alloreactive T-B cell interaction.
Agüeros, C; Arias, M; Benito, A; Cosme, LS; Gimenez, T; Gómez-Alamillo, C; Merino, J; Merino, R; Ramos-Barrón, MA; Santiuste, I, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (87)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's36 (41.38)18.2507
2000's47 (54.02)29.6817
2010's4 (4.60)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.61

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.61 (24.57)
Research Supply Index4.68 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (2.88%)5.53%
Reviews6 (5.77%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other95 (91.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]