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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: NELFINAVIRVIRACEPT (NELFINAVIR MESYLATE)
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 FDA : Bµî±Þ
(nelfinavir; )
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| º¸°ü»ó ÁÖÀÇ |
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| Ç׸ñ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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| Mechanism of Action |
Nelfinavir¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
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| Pharmacology |
Nelfinavir¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nelfinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
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| Metabolism |
Nelfinavir¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C19 (CYP2C19)Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2B6 (CYP2B6)
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| Protein Binding |
Nelfinavir¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >98%
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| Half-life |
Nelfinavir¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3.5 - 5 hours
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| Absorption |
Nelfinavir¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed following oral administration.
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| Pharmacokinetics |
NelfinavirÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö
À½½Ä°ú ÇÔ²² º¹¿ë ½Ã AUC: 2¹è ÀÌ»ó Áõ°¡
ÃÖ°í Ç÷Áß ³óµµ µµ´Þ ½Ã°£: 2-4½Ã°£
- ºÐÆ÷
ºÐÆ÷ ¿ëÀû (Vd): 2-7L/kg
- ´ë»ç
´Ü¹é °áÇÕ: 98%
°£ ´ë»ç È¿¼Ò: CYP3A3/4
¸ð¾à¹°º¸´Ù ÁÖ ´ë»ç¹°ÀÌ È°¼ºÀ» °¡Áø´Ù
- ¹è¼³
¼Ò½Ç ¹Ý°¨±â: 3.5~5½Ã°£
¹è¼³ °æ·Î ¹× ÇüÅ : º¯(98%~99%. 77%´Â ´ë»çü, 22%´Â ¹Ìº¯Èü), ´¢(1%~2%)
TOTAL BODY CLEARANCE: 1.05 L/hr/kg
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| Biotransformation |
Nelfinavir¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic via cytochrome P450 (CYP450) enzymes. CYP3A and CYP2C19 appear to be the predominant enzymes that metabolize nelfinavir in humans. One major and several minor metabolites are found in plasma; the major oxidative metabolite has in vitro antiviral activity comparable to that of the parent drug.
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| Toxicity |
Nelfinavir¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
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| Drug Interactions |
Nelfinavir¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alprazolam The protease inhibitor increases the effect of the benzodiazepineChlordiazepoxide The protease inhibitor increases the effect of the benzodiazepineClonazepam The protease inhibitor increases the effect of the benzodiazepineClorazepate The protease inhibitor increases the effect of the benzodiazepineCyclosporine The protease inhibitor increases the effect of cyclosporineDiazepam The protease inhibitor increases the effect of the benzodiazepineEletriptan The protease inhibitor increases the effect and toxicity of eletriptanEplerenone The protease inhibitor increases the effect and toxicity of eplerenoneEstazolam The protease inhibitor increases the effect of the benzodiazepineFentanyl The protease inhibitor increases the effect and toxicity of fentanylFlurazepam The protease inhibitor increases the effect of the benzodiazepineFusidic Acid The protease inhibitor increases the effect and toxicity of fusidic acidHalazepam The protease inhibitor increases the effect of the benzodiazepineMidazolam The protease inhibitor increases the effect of the benzodiazepinePrazepam The protease inhibitor increases the effect of the benzodiazepineQuazepam The protease inhibitor increases the effect of the benzodiazepineSildenafil The protease inhibitor increases the effect and toxicity of sildenafilTacrolimus The protease inhibitor increases the effect and toxicity of tacrolimusTriazolam The protease inhibitor increases the effect of the benzodiazepineVardenafil The protease inhibitor increases the effect and toxicity of vardenafilWarfarin The protease inhibitor increases the anticoagulant effectAcenocoumarol The protease inhibitor increases the anticoagulant effectDicumarol The protease inhibitor increases the anticoagulant effectAnisindione The protease inhibitor increases the anticoagulant effectAmiodarone Nelfinavir increases the effect and toxicity of amiodaroneAtorvastatin Nelfinavir increases the effect and toxicity of the statinDihydroergotamine Nelfinavir increases the effect and toxicity of ergot derivativeDihydroquinidine barbiturate Nelfinavir increases the effect and toxicity of quindineErgotamine Nelfinavir increases the effect and toxicity of ergot derivativeFelodipine Nelfinavir increases the effect and toxicity of felodipineLovastatin Nelfinavir increases the effect and toxicity of the statinMethadone Nelfinavir decreases the effect of methadoneNevirapine Nevirapine decreases the effect of nelfinavirPimozide Nelfinavir increases the effect and toxicity of pimozideQuinidine Nelfinavir increases the effect and toxicity of quinidineQuinidine barbiturate Nelfinavir increases the effect and toxicity of quinidineRanolazine Increased levels of ranolazine - risk of toxicityRifampin Rifampin decreases the effect of nelfinavirSimvastatin Nelfinavir increases the effect and toxicity of the statinSt. John's Wort St. John's Wort decreases the effect of indinavirSolifenacin This potent CYP3A4 inhibitor slows darifenacin / solifenacin metabolismDarifenacin This potent CYP3A4 inhibitor slows darifenacin / solifenacin metabolismSunitinib Possible increase in sunitinib levelsTerfenadine Increased risk of cardiotoxicity and arrhythmiasAstemizole Increased risk of cardiotoxicity and arrhythmiasCisapride Increased risk of cardiotoxicity and arrhythmiasAprepitant This CYP3A4 inhibitor increases the effect and toxicity of aprepitantCiclesonide Increased effects/toxicity of ciclesonideErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibEthinyl Estradiol Ritonavir could decrease the contraceptive efficacyMestranol Ritonavir could decrease the contraceptive efficacy
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Nelfinavir¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
erythromycin
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
**nelfinavir**
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
erythromycin
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Food Interaction |
Nelfinavir¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food.Food significantly increases absorption (2 to 3 times).
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| Drug Target |
[Drug Target]
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| Description |
Nelfinavir¿¡ ´ëÇÑ Description Á¤º¸ A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. [PubChem]
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| Dosage Form |
Nelfinavir¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Powder OralTablet Oral
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| Drug Category |
Nelfinavir¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-HIV AgentsHIV Protease Inhibitors
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| Smiles String Canonical |
Nelfinavir¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=C(C=CC=C1O)C(=O)NC(CSC1=CC=CC=C1)C(O)CN1CC2CCCCC2CC1C(=O)NC(C)(C)C
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| Smiles String Isomeric |
Nelfinavir¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC1=CC=CC=C1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C
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| InChI Identifier |
Nelfinavir¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C32H45N3O4S/c1-21-25(15-10-16-28(21)36)30(38)33-26(20-40-24-13-6-5-7-14-24)29(37)19-35-18-23-12-9-8-11-22(23)17-27(35)31(39)34-32(2,3)4/h5-7,10,13-16,22-23,26-27,29,36-37H,8-9,11-12,17-20H2,1-4H3,(H,33,38)(H,34,39)/t22-,23+,26-,27-,29+/m0/s1/f/h33-34H
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| Chemical IUPAC Name |
Nelfinavir¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide
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| Drug-Induced Toxicity Related Proteins |
NELFINAVIR ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Transcription factor AP-2 alpha;AP-2 complex subunit alpha-2;AP-2 complex subunit beta-1 Drug:nelfinavir Toxicity:lipodystrophy (fat redistribution favoring the accumulation of abdominal and cervical adipose tissue), hyperlipidemia, and insulin resistance. [¹Ù·Î°¡±â] Replated Protein:Lipoprotein lipase Drug:nelfinavir Toxicity:lipodystrophy (fat redistribution favoring the accumulation of abdominal and cervical adipose tissue), hyperlipidemia, and insulin resistance. [¹Ù·Î°¡±â] Replated Protein:Adiponectin Drug:nelfinavir Toxicity:lipodystrophy (fat redistribution favoring the accumulation of abdominal and cervical adipose tissue), hyperlipidemia, and insulin resistance. [¹Ù·Î°¡±â]
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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2021-12-09
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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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