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1. °¡Àӱ⠿©¼ºÀÇ ´ÙÀ½°ú °°Àº ¾Èµå·Î°Õ ÀÇÁ¸¼º ÁúȯÀÇ Ä¡·á
- Áߵ ¹× ÁßÁõ ¿©µå¸§(Áö·ç ¼ö¹Ý ¿©ºÎ¿Í °ü°è¾øÀÌ)
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2. ÀÌ ¾àÀº ¿©µå¸§ Ä¡·á¸¦ À§ÇØ ±¹¼Ò¼º Ä¡·áÁ¦ ¹× Àü½Å Ç×»ýÁ¦¸¦ ÀÌ¿ëÇÑ Ä¡·á°¡ ½ÇÆÐÇÑ ÀÌÈÄ¿¡¸¸ »ç¿ëµÇ¾î¾ß ÇÑ´Ù.
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ÀÌ ¾àÀ» Åõ¿©Çϱâ Àü¿¡ È£¸£¸óÀû ÇÇÀÓÁ¦ÀÇ »ç¿ëÀ» ÁßÁöÇÏ¿©¾ß ÇÑ´Ù. ÀÌ ¾àÀÇ ¿ë¹ýÀº È¥Çհ汸ÇÇÀÓÁ¦ÀÇ »ç¿ë¹ý°ú À¯»çÇϹǷΠµ¿ÀÏÇÏ°Ô Åõ¿©ÇÏ´Â °ÍÀ» °í·ÁÇØ¾ß ÇÑ´Ù.
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1. óÀ½ º¹¿ëÀ» ÇÒ °æ¿ì
1) Áö³´Þ È£¸£¸óÀû ÇÇÀÓÁ¦¸¦ »ç¿ë ¾ÈÇÑ °æ¿ì
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2) º¹ÇÕ È£¸£¸ó ÇÇÀÓÁ¦(º¹Çհ汸ÇÇÀÓÁ¦/COC, Áú¸µ, ȤÀº °æÇÇÆÐÄ¡Á¦)¿¡¼ ¹Ù²Ù´Â °æ¿ì
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3) ÇÁ·Î°Ô½ºÅ×·Ð ´ÜÀϼººÐ¸¸À» ÇÔÀ¯ÇÏ´Â ÇÇÀÓÁ¦¿¡¼ ¹Ù²Ù´Â °æ¿ì
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2. º¹¿ëÀ» ÀؾúÀ» °æ¿ì
1) º¹¿ëÇÒ ½Ã°£À¸·ÎºÎÅÍ 12½Ã°£À» °æ°úÇÏÁö ¾ÊÀº °æ¿ì
»ý°¢³ Áï½Ã 1Á¤À» º¹¿ëÇÏ°í Æò»ó½Ã´ë·Î Á¤ÇØÁø ½Ã°£¿¡ ´ÙÀ½ Á¤Á¦¸¦ º¹¿ëÇÑ´Ù.
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13) ¹ÝÃø ¸¶ºñ¼º ÆíµÎÅë ȯÀÚ ¶Ç´Â ±¹¼Ò ½Å°æ°è Áõ»óÀ» µ¿¹ÝÇÑ ÆíµÎÅëÀÇ º´·ÂÀÌ Àִ ȯÀÚ
14) ÃéÀå¿°À̳ª ½ÉÇÑ °úÆ®¸®±Û¸®¼¼¸®µåÇ÷Áõ°ú °ü·ÃµÈ º´·ÂÀ» °¡Áø ȯÀÚ
15) ÀÌ ¾àÀÇ ¾î¶°ÇÑ ¼ººÐ¿¡ ´ëÇØ ¾Ë·ÁÁø °ú¹ÎÁõÀÌ Àִ ȯÀÚ
16) ³²¼º
17) ÀÌ ¾àÀº À¯´çÀ» ÇÔÀ¯Çϰí ÀÖÀ¸¹Ç·Î, °¥¶ôÅä¿À½º ºÒ³»¼º(galactose intolerance), Lapp À¯´çºÐÇØÈ¿¼Ò °áÇÌÁõ(Lapp lactase deficiency) ¶Ç´Â Æ÷µµ´ç-°¥¶ôÅä¿À½º Èí¼öÀå¾Ö(glucose-galactose malabsorption) µîÀÇ À¯ÀüÀûÀÎ ¹®Á¦°¡ Àִ ȯÀÚ¿¡°Ô´Â Åõ¿©ÇÏ¸é ¾È µÈ´Ù.
18) Ãʰæ Àü ¿©¼º ¹× Æó°æ ÈÄ ¿©¼º
19) ´Ù¸¥ È£¸£¸ó¼º ÇÇÀÓÁ¦¸¦ º¹¿ëÇϴ ȯÀÚ
20) Á¤¸Æ¼º ¶Ç´Â µ¿¸Æ¼º Ç÷ÀüÁõ¿¡ ´ëÇÏ¿© ¼±ÃµÀû ¶Ç´Â ÈÄõÀû ¼ÒÀÎÀÌ Àִ ȯÀÚ (¿¹, Ȱ¼º´Ü¹éC (APC) ÀúÇ×¼º, ¾ÈƼƮ·Òºó-III °áÇÌ, ´Ü¹é C °áÇÌ, ´Ü¹é S °áÇÌ, hyperhomocysteinemia ¹× antiphospholipid Ç×ü (anticardiolipin Ç×ü, lupus anticoagulant))
21) ¼ö¸·Á¾ ¶Ç´Â ¼ö¸·Á¾ º´·ÂÀ» °¡Áø ȯÀÚ
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5) Á¤¸Æ·ù¼º Á¤¸ÆÀÌ Àִ ȯÀÚ
6) Á¤¸Æ¿°ÀÇ º´·ÂÀÌ Àִ ȯÀÚ
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±× ¿Ü ´ÙÀ½ÀÇ ÀÌ»ó¹ÝÀÀ(ÁßÁõ ÀÌ»ó¹ÝÀÀ Æ÷ÇÔ)ÀÌ º¹Çհ汸ÇÇÀÓ¾àÀ» º¹¿ëÇÏ´Â ¿©¼º¿¡°Ô¼ º¸°íµÇ¾úÀ¸¸ç, ÀÚ¼¼ÇÑ »çÇ×Àº ÀϹÝÀû ÁÖÀÇÇ×À» Âü°íÇÑ´Ù.
1) ½ÉÇ÷°ü°è: Á¤¸Æ°ú µ¿¸ÆÀÇ Ç÷Àü»öÀüÁúȯ, Ç÷¾Ð»ó½Â, °íÇ÷¾Ð, ³úÇ÷°ü »ç°í
2) ºñ´¢»ý½Ä±â°è: ¿ù°æ¿ÜÃâÇ÷(ÆÄźÃâÇ÷, Á¡»óÃâÇ÷), ¿ù°æ¾çÀÇ º¯È, °æºÎ ¹Ì¶õ°ú ÁúºÐºñ¹° º¯È, º¹¿ë±â°£À̳ª º¹¿ëÁßÁöÈÄ ¹«¿ù°æ, º¹¿ëÁßÁöÈÄ ¹«¹è¶õ, ÀڱñÙÁ¾Å©±âÀÇ Áõ°¡, ¿ëÇ÷¼º ¿äµ¶ÁõÈıº, ÀڱðæºÎ¾Ï
3) À¯¹æ : À¯¹æº¯È
4) ¼Òȱâ°è: º¹ºÎ °æ·Ã, ´ãÁ¤Ã¼¼º Ȳ´Þ ¶Ç´Â °¡·Á¿ò, ¾Ç¼º ¹× ¾ç¼º °£Á¾¾ç, °£±â´ÉÀå¾Ö, ´ã¼® Çü¼º, Æ÷¸£ÇǸ°Áõ, ¸¸¼º ¿°Áõ¼º ÀåÁúȯ(Å©·Ð¾¾º´), ±Ë¾ç´ëÀå¿°
5) ÁßÃ߽Űæ°è: ¿ì¿ïÁõ, Çö±â, Á¹À½, ½Ãµ§ÇÔ ¹«µµº´ (Sydenham's chorea)
6) ÇǺÎ: °¥»ö¹Ý, ¾Ë·¯Áö¼º È«¹Ý, ±¤°ú¹Î Áõ»ó, ¿øÇüÅ»¸ðÁõ, ¼Ò¾ç°¨, ±â¹Ì, Àü½Å¼º È«¹Ý¼º ·çǪ½º, Àӽů÷Áø
7) ±Í: À̰æÈÁõ °ü·Ã û°¢Àå¾Ö
8) ´ë»ç: ´ç³»¼º º¯È, ¸»ÃÊ Àν¶¸° ÀúÇ×¼º¿¡ ´ëÇÑ ¿µÇâ, °íÆ®¸®±Û¸®¼¼¸®µåÇ÷Áõ
9) ±âŸ: ½Ä¿åº¯È
10) À¯Àü¼º ¹× ÈÄõ¼º Ç÷°ü ºÎÁ¾ÀÌ ÀÖ´Â ¿©¼º¿¡°Ô Åõ¿©µÈ ¿ÜÀμº ¿¡½ºÆ®·Î°ÕÀº Ç÷°ü ºÎÁ¾ Áõ»óÀ» ¾ß±âÇϰųª ¾ÇȽÃų ¼ö ÀÖ´Ù.
11) Ç÷°ü°è : Ç÷Àü»öÀüÁõ(ÀÌ ¾àÀ» »ç¿ëÇÏ´Â ¿©¼ºÀÇ °æ¿ì Ç÷Àü»öÀüÁõÀÇ À§Ç輺ÀÌ Áõ°¡ÇÑ´Ù. ¹ß»ýºóµµ : µå¹² (1/10,000¿¡¼ 1/1,000))
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3) ÀÌ ¾àÀÇ Å¬¸®¾î·±½º¸¦ Áõ°¡½ÃŰ´Â ¾à¹°(È¿¼Ò À¯µµ¿¡ ÀÇÇÑ ÀÌ ¾àÀÇ È¿°ú °¨¼Ò)·Î Ç×Àü°£Á¦(Æä´ÏÅäÀÎ), ¹Ù¸£ºñÅ»·ù, ÇÁ¸®¹Ìµ·, Ä«¹Ù¸¶Á¦ÇÉ, ¸®ÆÊÇǽÅ, Æä´ÒºÎŸÁ¸ µîÀÌ ÀÖÀ¸¸ç, ¿Á½ºÄ«¹Ù¸¶Á¦ÇÉ, ÅäÇǶó¸ÞÀÌÆ®, Æç¹Ù¸ÞÀÌÆ®, ¸®Å䳪ºñ¸£, ±×¸®¼¼¿ÀÇ®ºó°ú ¼¼ÀÎÆ®Á¸½ºÇ®À» ÇÔÀ¯ÇÏ´Â ¹°Áú ¶ÇÇÑ ÀÌ·¯ÇÑ ¿µÇâÀÌ ÀÖÀ» ¼ö ÀÖ´Ù.
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5) ÀϺΠÇ×»ýÁ¦(¿¹, ¾ÏÇǽǸ°, Åׯ®¶ó½ÎÀÌŬ¸°)¿Í º´¿ë ÈÄ ÇÇÀÓÀÌ ½ÇÆÐÇÑ »ç·Ê°¡ º¸°íµÇ¾úÀ¸³ª, Á¤È®ÇÑ ±âÀüÀº ¹àÇôÁöÁö ¾Ê¾Ò´Ù.
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7)¡¡¿¡ÀÌÁî ¹× CÇü °£¿° ´Ü¹éÁú ºÐÇØÈ¿¼Ò ¾ïÁ¦Á¦(HIV/HCV protease inhibitor)¿Í ºñÇٻ꿪Àü»ç È¿¼Ò ÀúÇØÁ¦(non nucleoside reverse transcriptase inhibitor)¿Í º´¿ë½Ã ÀÌ ¾àÀÇ Å¬¸®¾î·±½º¿¡ ¿µÇâÀ» ¹ÌÃÄ ¿¡½ºÆ®·Î°Õ ¶Ç´Â ÇÁ·Î°Ô½ºÆ¾ÀÇ Ç÷Àå ³óµµ¸¦ Áõ°¡ ȤÀº °¨¼Ò½Ãų ¼ö ÀÖ´Ù. ÀÌ·¯ÇÑ º¯È´Â ÀϺΠ°æ¿ì¿¡ ÀÓ»óÀûÀ¸·Î °ü·ÃÀÌ ÀÖÀ» ¼ö ÀÖ´Ù.
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| Mechanism of Action |
Cyproterone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.
Estradiol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
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| Pharmacology |
Cyproterone¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cyproterone is an antiandrogen. It suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels).
Estradiol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
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| Metabolism |
Cyproterone¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
Estradiol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2A6 (CYP2A6)Glucuronosyltransferase
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| Protein Binding |
Estradiol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >95%
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| Half-life |
Cyproterone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Elimination Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.
Estradiol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 36 hours
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| Absorption |
Cyproterone¿¡ ´ëÇÑ Absorption Á¤º¸ Completely absorbed following oral administration.
Estradiol¿¡ ´ëÇÑ Absorption Á¤º¸ 43%
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| Biotransformation |
Cyproterone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. Cyproterone acetate is metabolized by the CYP3A4 enzyme, forming the active metabolite 15beta-hydroxycyproterone acetate, which retains its antiandrogen activity, but has reduced progestational activity.
Estradiol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.
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| Toxicity |
Cyproterone¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Estradiol¿¡ ´ëÇÑ Toxicity Á¤º¸ Can cause nausea and vomiting, and withdrawal bleeding may occur in females.
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| Drug Interactions |
Cyproterone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Estradiol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The enzyme inducer decreases the effect of hormonesAprobarbital The enzyme inducer decreases the effect of hormonesButabarbital The enzyme inducer decreases the effect of hormonesButalbital The enzyme inducer decreases the effect of hormonesButethal The enzyme inducer decreases the effect of hormonesEthotoin The enzyme inducer decreases the effect of hormonesFosphenytoin The enzyme inducer decreases the effect of hormonesGriseofulvin The enzyme inducer decreases the effect of hormonesHeptabarbital The enzyme inducer decreases the effect of hormonesHexobarbital The enzyme inducer decreases the effect of hormonesMephenytoin The enzyme inducer decreases the effect of hormonesMethohexital The enzyme inducer decreases the effect of hormonesMethylphenobarbital The enzyme inducer decreases the effect of hormonesPentobarbital The enzyme inducer decreases the effect of hormonesPhenobarbital The enzyme inducer decreases the effect of hormonesPhenytoin The enzyme inducer decreases the effect of hormonesPrednisolone The estrogenic agent increases the effect of corticosteroidPrednisone The estrogenic agent increases the effect of corticosteroidPrimidone The enzyme inducer decreases the effect of hormonesSecobarbital The enzyme inducer decreases the effect of hormonesTalbutal The enzyme inducer decreases the effect of hormonesRaloxifene Association not recommendedUrsodeoxycholic acid Estrogens decreases the effect of ursodiol
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Cyproterone¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take after a meal.Avoid alcohol.
Estradiol¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take with food to decrease nausea.
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| Drug Target |
[Drug Target]
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| Description |
Cyproterone¿¡ ´ëÇÑ Description Á¤º¸ An anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem]
Estradiol¿¡ ´ëÇÑ Description Á¤º¸ Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
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| Drug Category |
Cyproterone¿¡ ´ëÇÑ Drug_Category Á¤º¸ Androgen Antagonists
Estradiol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-menopausal AgentsAnticholesteremic AgentsEstrogens
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| Smiles String Canonical |
Cyproterone¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(=O)C1(O)CCC2C3C=C(Cl)C4=CC(=O)C5CC5C4(C)C3CCC12C
Estradiol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC12CCC3C(CCC4=C3C=CC(O)=C4)C1CCC2O
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| Smiles String Isomeric |
Cyproterone¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)[C@@H]5C[C@@H]5[C@]4(C)[C@H]3CC[C@]12C
Estradiol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C[C@]12CC[C@H]3[C@@H](CCC4=C3C=CC(O)=C4)[C@@H]1CC[C@@H]2O
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| InChI Identifier |
Cyproterone¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H27ClO3/c1-11(24)22(26)7-5-14-12-9-18(23)17-10-19(25)13-8-16(13)21(17,3)15(12)4-6-20(14,22)2/h9-10,12-16,26H,4-8H2,1-3H3/t12-,13+,14-,15-,16-,20-,21-,22-/m0/s1
Estradiol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
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| Chemical IUPAC Name |
Cyproterone¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
Estradiol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (8R,9S,13S,14S,17S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
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| Drug-Induced Toxicity Related Proteins |
CYPROTERONE ACETATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2B protein Drug:Cyproterone acetate Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:Heparin secretory transforming protein(HST) Drug:Cyproterone acetate Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] Replated Protein:CYP3A Drug:Cyproterone acetate Toxicity:idiosyncratic hepatotoxicity. [¹Ù·Î°¡±â] ESTRADIOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Myc proto-oncogene protein Drug:estradiol Toxicity:cytotoxic responses . [¹Ù·Î°¡±â] Replated Protein:3-hydroxy-3-methylglutaryl-coenzyme A reductase Drug:estradiol Toxicity:stimulate steroidogenesis. [¹Ù·Î°¡±â] Replated Protein:Stromelysin-2 Drug:estradiol Toxicity:nonbacterial prostatitis. [¹Ù·Î°¡±â] Replated Protein:Transcription factor E2F1 Drug:estradiol Toxicity:cytotoxic responses. [¹Ù·Î°¡±â] Replated Protein:Glucocorticoid receptor Drug:estradiol Toxicity:glucocorticoid resistance. [¹Ù·Î°¡±â]
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