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Estrogen-Only Menopausal Therapy

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Estrogen-Only Menopausal Therapy PHARMACEUTICALS volume 100 A A review of humAn cArcinogens This publication represents the views and expert opinions of an IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, which met in Lyon, 14-21 October 2008 LYON, FRANCE - 2012 iArc monogrAphs on the evAluAtion of cArcinogenic risks to humAns ESTROGEN-ONLY MENOPAUSAL THERAPY Estrogen therapy was considered by previous IARC Working Groups in 1987 and 1998 (IARC, 1987, 1999). Since that time, new data have become available, these have been incorpo- rated into the Monograph, and taken into consideration in the present evaluation. 1. Exposure Data (i) Structural and molecular formulae, and molecular mass 1.1 Identification of the agents O CH3 1.1.1 Conjugated estrogens H The term ‘conjugated estrogens’ refers to mixtures of at least eight compounds, including HH sodium estrone sulfate and sodium equilin sulfate, derived wholly or in part from equine NaO3SO urine or synthetically from estrone and equilin. Conjugated estrogens contain as concomitant C18H21O5S.Na components the sodium sulfate conjugates of Relative molecular mass: 372.4 17α-dihydroequilin, 17β-dihydroequilin, and (b) Sodium equilin sulfate 17α-estradiol (United States Pharmacopeial Convention, 2007). Chem. Abstr. Serv. Reg. No.: 16680-47-0 Chem. Abstr. Name: 3-(Sulfooxy)-estra- (a) Sodium estrone sulfate 1,3,5(10),7-tetraen-17-one, sodium salt Chem. Abstr. Serv. Reg. No.: 438-67-5 IUPAC Systematic Name: Sodium (13-methyl-17-oxo-9,11,12,14,15,16-hexa- Chem. Abstr. Name: 3-(Sulfooxy)-estra- hydro-6H-cyclopenta[a]phenanthren-3-yl) 1,3,5(10)-trien-17-one, sodium salt sulfate IUPAC Systematic Name: Sodium Synonyms: Equilin, sulfate, sodium salt; [(8R,9S,13S,14S)-13-methyl-17-oxo- equilin sodium sulfate; sodium equilin 7,8,9,11,12,14,15,16-octahydro-6H- 3-monosulfate cyclopenta[a]phenanthren-3-yl] sulfate Description: buff-coloured amorphous pow- Synonyms: Estrone sodium sulfate; estrone der, odourless or with a slight characteristic sulfate sodium; estrone sulfate sodium salt; odour [when obtained from natural sourc- oestrone sodium sulfate; oestrone sul- es]; white to light-buff-coloured crystalline fate sodium; oestrone sulfate sodium salt; or amorphous powder, odourless or with a sodium estrone sulfate; sodium estrone- slight odour [synthetic form] (Sweetman, 3-sulfate; sodium oestrone-3-sulfate 219 IARC MONOGRAPHS – 100A 2008) 1.1.3 Mestranol (i) Structural and molecular formulae, and Chem. Abstr. Serv. Reg. No.: 72-33-3 molecular mass Chem. Abstr. Name: (17α)-3-Methoxy-19- O norpregna-1,3,5(10)-trien-20-yn-17-ol CH3 IUPAC Systematic Name: (8R,9S,13S,14S,17R)-17-Ethynyl-3-me- thoxy-13-methyl-7,8,9,11,12,14,15,16-octa- hydro-6H-cyclopenta[a]phenanthren-17-ol HH Synonyms: Ethinylestradiol 3-methyl ether; 17α-ethinylestradiol 3-methyl NaO3SO ether; ethinyloestradiol 3-methyl ether; 17α-ethinyloestradiol 3-methyl ether; C18H19O5S.Na ethynylestradiol methyl ether; ethynyl- Relative molecular mass: 370.4 estradiol 3-methyl ether; 17-ethynylestra- diol 3-methyl ether; 17α-ethynylestradiol 1.1.2 Ethinylestradiol 3-methyl ether; 17α-ethynylestradiol methyl ether; ethynyloestradiol meth- Chem. Abstr. Serv. Reg. No.: 57-63-6 yl ether; ethynyloestradiol 3-methyl Chem. Abstr. Name: (17α)-19-Norpregna- ether; 17-ethynyloestradiol 3-methyl 1,3,5(10)-trien-20-yne-3,17-diol ether; 17α-ethynyloestradiol 3-methyl IUPAC Systematic Name: ether; 17α-ethynyloestradiol methyl (8R,9S,13S,14S,17R)-17-Ethynyl-13-meth- ether; 3-methoxy-17α-ethinylestradiol; yl-7,8,9,11,12,14,15,16-octahydro-6H- 3-methoxy-17α-ethinyloestradiol; cyclopenta[a]phenanthrene-3,17-diol 3-methoxy-17α-ethynylestradiol; 3-me- Synonyms: 17-Ethinyl-3,17-estradiol; thoxyethynylestradiol; 3-methoxy-17α- ethynyloestradiol; 3-methoxyethyny- 17-ethinylestradiol; 17α-ethinyl- loestradiol; 3-methylethynylestradiol; 17β-estradiol; ethinylestradiol; 3-O-methylethynylestradiol; 3-methylethy- 17α-ethinylestradiol nyloestradiol; 3-O-methylethynyloestradiol; Description: White to creamy- or slightly ∆-MVE yellowish-white, odourless, crystalline pow- Description: White or almost white to der (Sweetman, 2008) creamy-white, odourless, crystalline pow- der (Sweetman, 2008) (a) Structural and molecular formulae, and relative molecular mass (a) Structural and molecular formulae, and OH relative molecular mass CH3 OH C CH CH3 H C CH H HH HH HO H 3CO C20H24O2 Relative molecular mass: 296.4 C21H26O2 Relative molecular mass: 310.4 220 Estrogen-only menopausal therapy 1.1.4 Estradiol 17β-estradiol benzoate; 17β-estradiol 3-benzoate; estradiol monobenzoate; Chem. Abstr. Serv. Reg. No.: 50-28-2 1,3,5(10)-estratriene-3,17β-diol 3-benzo- Chem. Abstr. Name: (17β)-Estra-1,3,5(10)- ate; β-oestradiol benzoate; β-oestradiol triene-3,17-diol 3 benzoate; 17β-oestradiol benzoate; IUPAC Systematic Name: 17β-oestradiol 3-benzoate; oestradiol (8R,9S,13S,14S,17S)-13-Meth- monobenzoate; 1,3,5(10)-oestratriene- yl-6,7,8,9,11,12,14,15,16,17- 3,17β-diol 3-benzoate decahydrocyclopenta[a]phenan- Description: Almost white crystalline pow- threne-3,17-diol der or colourless crystal (Sweetman, 2008) Synonyms: Dihydrofollicular hormone; dihydrofolliculin; dihydromenfor- (a) Structural and molecular formulae, and mon; dihydrotheelin; dihydroxyestrin; relative molecular mass 3,17β-dihydroxyestra-1,3,5(10)-triene; OH 3,17-epidihydroxyestratriene; β-estradiol; CH3 17β-estradiol; 3,17β-estradiol; (d)-3,17β- H estradiol; oestradiol-17β; 17β-oestradiol H Description: White or creamy-white, odour- less, crystalline powder (Sweetman, 2008) O HH (a) Structural and molecular formulae, and C O relative molecular mass OH CH3 C25H28O3 H Relative molecular mass: 376.5 H 1.1.6 Estradiol cypionate HH Chem. Abstr. Serv. Reg. No.: 313-06-4 HO Chem. Abstr. Name: (17β)-Estra-1,3,5(10)- triene-3,17-diol, 17-cyclopentanepropano- C18H24O2 ate Relative molecular mass: 272.4 IUPAC Systematic Name: [(8R,9S,13S,14S,17S)-3-Hydroxy- 1.1.5 Estradiol benzoate 13-methyl-6,7,8,9,11,12,14,15,16,17- decahydrocyclopenta[a]phenanthren-17-yl] Chem. Abstr. Serv. Reg. No.: 50-50-0 3- cyclopentylpropanoate Chem. Abstr. Name: Estra-1,3,5(10)-triene- Synonyms: Cyclopentanepropionic acid, 3,17β-diol, 3-benzoate 17-ester with oestradiol; cyclopentanepro- IUPAC Systematic Name: pionic acid, 3-hydroxyestra-1,3,5(10)- [(8R,9S,13S,14S,17S)-17-Hydroxy- trien-17β-yl ester; depo-estradiol cyclo- 13-methyl-6,7,8,9,11,12,14,15,16,17- pentylpropionate; depoestradiol cypionate; decahydrocyclopenta[a]phenanthren-3-yl] estradiol 17β-cyclopentanepropionate; benzoate estradiol cyclopentylpropionate; estra- Synonyms: Estradiol benzoate; β-estradiol diol 17-cyclopentylpropionate; estradiol benzoate; β-estradiol 3-benzoate; 221 IARC MONOGRAPHS – 100A 17β-cyclopentylpropionate; 17β-estradiol (a) Structural and molecular formulae, and 17-cyclopentyl-propionate; estradiol cy- relative molecular mass pionate; estradiol 17-cypionate; estradiol O 17β-cypionate O C Description: White to practically white crys- CH3 H talline powder, odourless or with a slight CH3 odour (Sweetman, 2008) H (a) Structural and molecular formulae, and HH relative molecular mass HO O C23H32O3 O C CH3 Relative molecular mass: 356.5 H H 1.1.8 Estriol Chem. Abstr. Serv. Reg. No.: 50-27-1 HH Chem. Abstr. Name: (16α,17β)-Estra- HO 1,3,5(10)-triene-3,16,17-triol IUPAC Systematic Name: C H O 26 36 3 (8R,9S,13S,14S,16R,17R)-13-Meth- Relative molecular mass: 396.6 yl-6,7,8,9,11,12,14,15,16,17- decahydrocyclopenta[a]phenanthrene- 1.1.7 Estradiol valerate 3,16,17-triol Chem. Abstr. Serv. Reg. No.: 979-32-8 Synonyms: Estra-1,3,5(10)-triene- Chem. Abstr. Name: (17β)-Estra-1,3,5(10)- 3,16α,17β-triol; estratriol; 16α-estriol; triene-3,17-diol, 17-pentanoate 16α,17β-estriol; 3,16α,17β-estriol; follicular IUPAC Systematic Name: hormone hydrate; 16α-hydroxyestradiol; [(8R,9S,13S,14S,17S)-3-Hydroxy- 3,16α,17β-trihydroxyestra-1,3,5(10)-triene; 13-methyl-6,7,8,9,11,12,14,15,16,17- trihydroxyestrin decahydrocyclopenta[a]phenanthren-17-yl] Description: White or practically white, pentanoate odourless, crystalline powder (Sweetman, Synonyms: Oestradiol valerate; estradiol 2008) 17β-valerate; estradiol valerianate; estra- (a) Structural and molecular formulae and 1,3,5(10)-triene-3,17β-diol 17-valerate; relative molecular mass 3-hydroxy-17β-valeroyloxyestra-1,3,5(10)- OH CH triene 3 H Description: White or almost white crystal- line powder or colourless crystal, odour- H H less or with a faint fatty odour (Sweetman, OH 2008) HH HO C18H24O3 Relative molecular mass: 288.4 222 Estrogen-only menopausal therapy 1.1.9 Estrone (a) Structural and molecular formulae, and relative molecular mass Chem. Abstr. Serv. Reg. No.: 53-16-7 O Chem. Abstr. Name: 3-Hydroxyestra- CH3 1,3,5(10)-trien-17-one IUPAC Systematic Name: (8R,9S,13S,14S)- H + 3-Hydroxy-13-methyl-7,8,9,11,12,14,15,16- NH2 O HH octahydro-6H- cyclopenta[a]phenanthren- HN 17-one -O S O Synonyms: d-Estrone; d-oestrone O Description: Odourless, small white crystals C H N O S or white to creamy-white crystalline pow- 22 32 2 5 der (Sweetman, 2008) Relative molecular mass: 436.6 (a) Structural and molecular formulae, and relative molecular mass 1.2 Use of the agents O Information for Section 1.2 is taken from CH3 IARC (1999) and McEvoy (2007). H 1.2.1 Indications HH Menopausal estrogen therapy refers to the use of estrogen without a progestogen for women HO in the period around the menopause, primarily for the treatment of menopausal symptoms C18H22O2 Relative molecular mass: 270.4 but also for the prevention of conditions that become more common in the postmenopausal 1.1.10 Estropipate period, such as osteoporosis and ischaemic heart Chem. Abstr. Serv. Reg. No.: 7280-37-7 disease. It is mainly given to women who have Chem.
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