Roflumille 丨 cas 162401-32-3

Roflumille 丨 cas 162401-32-3yog aCov neeg xaiv tau yooj yim ntawm phosphodiesters -4 (pde4), ib qho enzyme uas tawg cia cyclic adenosine monophosphate (pw pem roob) Hauv cov hlab ntsha mob. Los ntawm kev tsim tsa lub chaw pw hav zoov sab nraud, roflumilletxo qhov mob o-particularly nyob rau hauv cov hlab-thiab tau pom zoo rau lubKev kho mob ntawm cov kab mob ntsws sib deev (CopD).

Raws li ib tugQhov ncauj tiv thaiv-inflammatory, roflumilast muab cov ntawv tshiab,Tsis yog-steroidal kho kev xaivQhov ntawd ua kom tiav pob pob pob thiab lwm cov tshuaj copd.

1. Cov kab mob sib tw ua rau lub ntsws (Copmonary)

Thawj Taw Qhiarau txo qhov kev pheej hmoo ntawmCOPD exacerbationsHauv cov neeg mob nrog:

Loj copd (fev1 <50%)

Mob qaib mob ntsws ntev phalotype

Keeb kwm ntawm cov nquag exacerbations

Lub tshuab: PDE4 inhibition ua rau nce chaw pw hauv ne

2. Asthma (tshawb xyuas)

Kawm siv rau hauvmob hawb pob, tshwj xeeb tshaj yog phenotypes nrog eosinophilic lossis neutrophilic o.

Qhia cov lus cog tseg hauv kev sib xyaw nrog kev kho mob nrog corticosteroids.

3. Lwm lwm cov mob cuam tshuam (preclinical \/ Kev Tshawb Fawb)

Raug tshawb nrhiav kom muaj peev xwm nyob rau hauv:

Pororiasis

Pulmonary Fibrosis

Inflammatory bowel kab mob (IBD)

Neuroinflammammammammatatory tej yamxws li ntau sclerosis lossis Alzheimer tus kab mob

1. Xaiv PDE4 Inhibition

Roflumilast 丨 cas 162401-32-3}} muajLub hom phiaj tiv thaiv kev tawm tsamHauv lub ntsws tsis muaj feem cuam tshuam PDE1-3 lossis PDE5 txoj hauv kev.

TxoAirway neutrophilic o, ua kom tus mob siab ntsws.

2. Qhov ncauj ib zaug-txhua hnub noj

Yooj yimNtsiav Tshuaj Ntsiav Tshuaj, feem ntau yog 500 μg ib zaug txhua hnub, txhim kho tus neeg mob ua kom muaj kev mob siab rau nqus tau.

3. Steroid-sparing muaj peev xwm

Tsis-corticosteroid anti-inflammatory kev puas tsuaj txo kev cia siab raunqus tau los yog lub kaw lus corticosteroids, uas muaj ntau cov kev mob tshwm sim ntxiv.

4. Exacerbation Txo Kev Pheej

Pom kev ua tau zoo hauv kev txo qisCov Ntawv Qhia Txog Coperate, tshwj xeeb tshaj yog nyob rau hauv cov neeg mob pheej hmoo nrog mob ntsws ntev.

Siab qhov ncauj bioavailability (~80%)

Ib nrab-lub neej: ~ 17 teev (txhawb nqa ib zaug noj tshuaj)

Cov metabolite nquag: Roflumilast N-Oxide (lub luag haujlwm rau ~ 90% ntawm PDE4 Inhibition)

Metabolized los ntawmCyp3a4 thiab cyp1a2

Roflumille 丨 cas 162401-32-3yog aXaiv PDE4 inhibitorsiv feem ntau rautiv thaiv cov tshuab luam ntawvHauv cov neeg mob uas mob ntsws ntev. Nrog nwstsis-steroidal, anti-inflammatoryismism, nws muaj kev sib cav sib txawv thiab kev kho kom zoo rauCov tub ceev xwm loj, nquag-exacerbatorCov. Kev tshawb fawb txuas ntxiv rau hauvmob hawb pob thiab mob kab mobtej zaum yuav nthuav nws cov chaw kho mob.