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Total database: 17430
Struktur (SMILES)
17 (65.4%)
Target
19 (73.1%)
Genomik
2 (7.7%)
Referensi
26 (100.0%)

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Hasil Pencarian (26)

small molecule | CAS: 238074-89-0

CH-1504 is a an antirheumatic agent that has been shown in vitro to be a nonpolyglutamylatable and nonhydroxylatable antifolate that is more efficiently taken up into cells by the reduced folate carrier (RFC) system than is Methotrexate. It has been investiga…

Kategori:
Heterocyclic Compounds, Fused-RingPteridinesPterins
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Aminopterin DB08878
small molecule | CAS: 54-62-6

Aminopterin is an amino derivative of folic acid, which was once used as an antineoplastic agent in the treatment of pediatric leukemia. In the 1950's its production was discontinued in favor of methotrexate, which is less potent but less toxic. Off label, am…

Kategori:
Enzyme InhibitorsFolic Acid AntagonistsHeterocyclic Compounds, Fused-Ring +2
Target Protein:
Peptide deformylase, mitochondrial
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Anifrolumab Approved DB11976
biotech | CAS: 1326232-46-5

Anifrolumab, or MEDI-546, is a type 1 interferon receptor (IFNAR) inhibiting IgG1? monoclonal antibody indicated in the treatment of adults with moderate to severe systemic lupus erythematosus.[A237074,L34929] The standard therapy for systemic lupus erythemat…

Kategori:
Amino Acids, Peptides, and ProteinsAntibodiesAntibodies, Monoclonal +10
Target Protein:
Interferon alpha/beta receptor 1
Waktu ParuhThe serum eliminati…
Vol. DistribusiBased on population…
KlirensFollowing the admin…
Genetik -
Aurothioglucose Approved DB09121
small molecule | CAS: 12192-57-3

Aurothioglucose, also known as gold thioglucose, was formerly used to treat rheumatoid arthritis. Contemporary research on the effect of gold salts treatment began in 1935, primarily to reduce inflammation and to slow disease progression in patients with r…

Kategori:
Antiinflammatory and Antirheumatic ProductsAntirheumatic AgentsDrugs that are Mainly Renally Excreted +5
Target Protein:
Adenylate cyclase type 1Adenylate cyclase type 2Adenylate cyclase type 5
Waktu ParuhThe biological half…
Vol. DistribusiReadily accessible …
KlirensWhen a standard wee…
Genetik -
Bevifimod DB15301
biotech | CAS: 2223113-32-2

Bevifimod is under investigation in clinical trial NCT01749787 (Safety Study of PRTX-100 With Methotrexate or Leflunomide to Treat Active Rheumatoid Arthritis).

Kategori:
Amino Acids, Peptides, and ProteinsAntigensAntigens, Bacterial +3
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
small molecule | CAS: 64425-90-7

Choline magnesium trisalicylate is a non-acetylated salicylate used widely as a nonsteroidal anti-inflammatory drug. Trisalicylate significantly reduces methotrexate renal clearance, displacing methotrexate from protein, increasing the fraction unbound by 28%…

Kategori:
Acids, CarbocyclicAgents causing hyperkalemiaAgents that produce hypertension +23
Target Protein:
Prostaglandin G/H synthase 1Prostaglandin G/H synthase 2
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
CR6086 DB16111
small molecule | CAS: 1417742-86-9

CR6086 is under investigation in clinical trial NCT03163966 (A Study of the EP4 Antagonist CR6086 in Combination With Methotrexate, in Dmard-naïve Patients With Early Rheumatoid Arthritis).

Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Dilmapimod DB12140
small molecule | CAS: 444606-18-2

Dilmapimod has been used in trials studying the treatment and diagnostic of Nerve Trauma, Inflammation, Pain, Neuropathic, Arthritis, Rheumatoid, and Coronary Heart Disease, among others. Dilmapimod (SB-681323) is a p38 MAP-kinase inhibitor that has potential…

Kategori:
p38 Mitogen-Activated Protein Kinases, antagonists & inhibitorsPyridines
Target Protein:
Mitogen-activated protein kinase 14Tumor necrosis factorInterleukin-1 beta +1
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Filgotinib Approved DB14845
small molecule | CAS: 1206161-97-8

Rheumatoid arthritis (RA) is a chronic, autoimmune, systemic, and inflammatory disease that causes synovial joint symptoms and can limit range of motion in severe cases.[A221451,A221456] The disease is associated with extra-articular manifestations, progressi…

Kategori:
Antineoplastic and Immunomodulating AgentsArthritis, Rheumatoid, drug therapyImmunosuppressive Agents +5
Target Protein:
Tyrosine-protein kinase JAK1
Waktu ParuhThe half-life of fi…
Vol. Distribusi-
Klirens-
Genetik -
Glucarpidase Approved DB08898
biotech | CAS: 9074-87-7

Glucarpidase is a recombinant carboxypeptidase G2 produced by genetically modified _Escherichia coli_ bacteria. It is a 390-amino acid homodimer protein.[L39855] High-dose [methotrexate], an antifolate agent, has been widely and safely used for many decades i…

Kategori:
Amino Acids, Peptides, and ProteinsAntidotesCarboxypeptidases +8
Waktu ParuhFollowing intraveno…
Vol. DistribusiIn healthy adults w…
KlirensThe mean systemic c…
Genetik -
Golimumab Approved DB06674
biotech | CAS: 476181-74-5

Golimumab is a human IgG1? monoclonal antibody derived from immunizing genetically engineered mice with human TNF?. Golimumab binds and inhibits soluble and transmembrane human TNF?. Increased TNF? is associated with chronic inflammation. Thus golimumab is in…

Kategori:
Agents reducing cytokine levelsAmino Acids, Peptides, and ProteinsAnti-Inflammatory Agents +17
Target Protein:
Tumor necrosis factor
Waktu ParuhGolimumab has a lon…
Vol. DistribusiAfter IV administra…
KlirensAfter one IV dose o…
Genetik -
Infliximab Approved DB00065
biotech | CAS: 170277-31-3

Infliximab is a tumor necrosis factor (TNF-alpha or TNF-?) blocker and a chimeric monoclonal IgG1 antibody composed of human constant (75%) and murine variable (25%) regions [A31469]. Infliximab is produced by a recombinant cell line cultured by continuous pe…

Kategori:
Agents Causing Muscle ToxicityAgents reducing cytokine levelsAmino Acids, Peptides, and Proteins +21
Target Protein:
Tumor necrosis factor
Gen Terkait:
FCGR3A
Waktu ParuhThe median terminal…
Vol. DistribusiBased on a pharmaco…
KlirensIn patients with Cr…
Genetik 1 Varian
JNJ-39758979 DB18899
small molecule | CAS: 1046447-90-8

JNJ-39758979 is under investigation in clinical trial NCT01480388 (A Dose Range Finding Study of JNJ-39758979 in Patients With Active Rheumatoid Arthritis Currently Treated With Methotrexate).

Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Leucovorin Approved DB00650
small molecule | CAS: 58-05-9

Folinic Acid (also known as 5-formyl tetrahydrofolic acid or leucovorin) is the 5-formyl derivative of tetrahydrofolic acid, a necessary co-factor in the body. Commercially available leucovorin is composed of a 1:1 racemic mixture of the dextrorotary and levo…

Kategori:
AntidotesCoenzymesCompounds used in a research, industrial, or household setting +15
Target Protein:
Proton-coupled folate transporterDihydrofolate reductase
Waktu Paruh6.2 hours
Vol. Distribusi-
Klirens-
Genetik -
Levilimab DB16387
biotech | CAS: 2035008-70-7

Levilimab is under investigation in clinical trial NCT04227366 (Study of the Efficacy and Safety of BCD-089 in Combination With Methotrexate in Patients With Active Rheumatoid Arthritis).

Kategori:
Amino Acids, Peptides, and ProteinsAntibodiesAntibodies, Monoclonal +9
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Levoleucovorin Approved DB11596
small molecule | CAS: 68538-85-2

Levoleucovorin is the enantiomerically active form of Folinic Acid (also known as 5-formyl tetrahydrofolic acid or leucovorin). Commercially available leucovorin is composed of a 1:1 racemic mixture of the dextrorotary and levorotary isomers, while levoleucov…

Kategori:
AntidotesCoenzymesCompounds used in a research, industrial, or household setting +14
Target Protein:
Serine hydroxymethyltransferase
Waktu ParuhThe mean terminal h…
Vol. DistribusiData can't be found.
KlirensData can't be found.
Genetik -
Methopterin DB16620
small molecule | CAS: 2410-93-7

Methopterin is thought to have effects on osteoclasts and to inhibit inflammatory bone destruction.[A229843]

Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -
Methotrexate Approved DB00563
small molecule | CAS: 59-05-2

Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis.[A180322] This inhibition leads to suppression of inflammation as well as prevention of cell division.[A180322] Because of these effects, methotrexate is of…

Kategori:
Abortifacient AgentsAbortifacient Agents, NonsteroidalAgents Causing Muscle Toxicity +42
Target Protein:
Thymidylate synthaseReduced folate transporterProton-coupled folate transporter +2
Gen Terkait:
ABCC2 MTHFR
Waktu ParuhThe half life of lo…
Vol. DistribusiThe volume of distr…
KlirensMethotrexate cleara…
Genetik 2 Varian
Mifamurtide Approved DB13615
small molecule | CAS: 83461-56-7

Mifamurtide is an immunomodulator with antitumor activity via activation of macrophages and monocytes. Also called L-MTP-PE, mifamurtide may be a liposomal form of of the active ingredient MTP-PE, which is a synthetic, less pyrogenic, and longer-acting deriva…

Kategori:
Adjuvants, ImmunologicAmino Acids, Peptides, and ProteinsAmino Sugars +15
Target Protein:
Toll-like receptor 4Nucleotide-binding oligomerization domain-containing protein 2
Waktu ParuhFollowing intraveno…
Vol. DistribusiThe mean volume of …
KlirensThe clearance from …
Genetik -
Pegloticase Approved DB09208
biotech | CAS: 885051-90-1

Pegloticase is a porcine recombinant PEGylated uricase indicated for the treatment of chronic gout in adult patients that do not respond to other types of therapies.[L42425] Pegloticase has a similar activity to rasburicase, an enzyme that metabolizes uric ac…

Kategori:
Antigout PreparationsCompounds used in a research, industrial, or household settingEnzymes +6
Target Protein:
Uric acid
Waktu ParuhIn patients with sy…
Vol. DistribusiThe volume of distr…
KlirensIn gout patients gi…
Genetik -
Pralatrexate Approved DB06813
small molecule | CAS: 146464-95-1

Pralatrexate is an antifolate for the treatment of relapsed or refractory peripheral T-cell lymphoma [L37674]. Pralatrexate was developed in response due to the inferior responses of patients using the standard therapy for their B-cells counterparts.[A246693]…

Kategori:
AntimetabolitesAntineoplastic AgentsAntineoplastic and Immunomodulating Agents +10
Target Protein:
Dihydrofolate reductasePeptide deformylase, mitochondrialFolylpolyglutamate synthase, mitochondrial +1
Waktu ParuhThe terminal elimin…
Vol. DistribusiThe steady-state vo…
KlirensThe total systemic …
Genetik -
Sarilumab Approved DB11767
biotech | CAS: 1189541-98-7

Sarilumab is a fully human anti-interleukin 6 (IL-6) receptor monoclonal IgG1 antibody that binds to both membrane-bound and soluble IL-6 receptor forms, thus blocking the cis- and trans-inflammatory signalling cascades of IL-6.[A27262] Sarilumab was develope…

Kategori:
Amino Acids, Peptides, and ProteinsAntibodiesAntibodies, Monoclonal +22
Target Protein:
Interleukin-6 receptor subunit alphaHigh affinity immunoglobulin gamma Fc receptor ILow affinity immunoglobulin gamma Fc region receptor II-a +3
Waktu ParuhThe half-life will …
Vol. DistribusiIn patients with rh…
KlirensSarilumab is not el…
Genetik -
Sulfasalazine Approved DB00795
small molecule | CAS: 599-79-1

Sulfasalazine is an anti-inflammatory drug structurally related to salicylates and other non-steroidal anti-inflammatory drugs. It is indicated for managing inflammatory diseases such as ulcerative colitis and rheumatoid arthritis (RA).[L39065, A255582] Metab…

Kategori:
Agents causing hyperkalemiaAgents that produce hypertensionAlimentary Tract and Metabolism +23
Target Protein:
Broad substrate specificity ATP-binding cassette transporter ABCG2Transcription factor RelBTranscription factor p65 +12
Waktu ParuhThe observed plasma…
Vol. DistribusiFollowing intraveno…
KlirensThe calculated clea…
Genetik -
Tofacitinib Approved DB08895
small molecule | CAS: 477600-75-2

Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds…

Kategori:
Antineoplastic and Immunomodulating AgentsAntirheumatic AgentsBiologics for Rheumatoid Arthritis Treatment +14
Target Protein:
Tyrosine-protein kinase JAK1Tyrosine-protein kinase JAK2Tyrosine-protein kinase JAK3 +1
Waktu Paruh~3 hours
Vol. DistribusiVd= 87L after intra…
Klirens-
Genetik -
Ustekinumab Approved DB05679
biotech | CAS: 815610-63-0

Ustekinumab is a human immunoglobulin (Ig) G1 kappa monoclonal antibody directed against interleukin(IL)-12 and IL-23, which are cytokines that are involved in immune and inflammatory responses.[A187349] It was generated via recombinant human IL-12 immunizati…

Kategori:
Amino Acids, Peptides, and ProteinsAntibodiesAntibodies, Monoclonal +16
Target Protein:
Interleukin-23Interleukin-12 subunit beta
Waktu ParuhFollowing administr…
Vol. DistribusiThe total volume of…
KlirensThe median apparent…
Genetik -
VX-702 DB05470
small molecule | CAS: 745833-23-2

VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA). It acts as a p38 MAP kinase inhibitor. In the future, VX-702 may be investigated for combination with methotr…

Kategori:
AmidesBenzene Derivatives
Target Protein:
Mitogen-activated protein kinase 14Tumor necrosis factorInterleukin-1 beta +1
Waktu Paruh-
Vol. Distribusi-
Klirens-
Genetik -