1186 Bone

Lasofoxifene Ta rtrate (BANM, USAN r/NNM) 0 Minodronate Profile CP-336156(8: Lasofoxifene, Tartrate de; Lasofoxifeni Tartras; is a cathepsin-K inhibitor that reduces bone TartriHo de lasofoxifeno; f!a3o¢oKc'1$eHa TaprpaT: (r/NN) resorption. It is being investigated for the treatment of (+c;;;-5,6,7,1;cJetra hydro-6-pheny!-5.-{pc[2-.(1 -pyrrglidinyi) . Acide Mlnodronicjue; 1\cido minQdr6nlco; . Acidum minqc ethmy]pheny!�2-napht�ol Q-tartrate (1:1 ). •. References. 2 2 MwHo/!po�oBaR I. Bone HG, et a!. Odanacatib, a cathepsin-K inhibitor for osteoporosis: a c,,H,,N0:/:4H<>O,�S61,6 011()-59 0; YH-5 9; • YM"S29; ••.• �����:aT ;·_. study in postmenopausal women with low bone density. J CAS--· 790l9 1 -29�R Res 2009; 25: 937---47. ( 1 ·Hydroxy•2•imipazo[1 ,2:a]pyridin-3-ylethyiidene)dipho- ATC G03Xt03 . · 2. Lewiecki EM. Odanacatib, a inhibitor for the treatment of sphonicacid. · . . osteoporosis and other skeletal disorders associated with excessive bone C9 H,2N2G.h,•3;1.4:.1 remodeling. !Drugs 2009; 12: 799-809. UNII (45 � 12765J'4Jo5 NOTE. The name Fablyn has been used as a trade mark lor UNIJ �·40SG.R63TGt lasofoxifene tartrate. Oxidronate Profile Profile Minodronate is a that inhibits bone Lasofoxifene is a selective oestrogen receptor modulator resorption. It is given as minodronic acid hydrate for the similar to raloxifene (p. 2303.1 ), that was developed lor the treatment of osteoporosis; l mg is given orally once daily, treatment of osteoporosis in postmenopausal women at usually in the morning. Specific instructions for oral use increased risk of fracture. (see Precautions in Alendronate, p. ll72.3) should be References. followed to minimise adverse effects and permit adequate 1. Gennari L. Lasofoxifene, a new selective estrogen receptor modulator for absorption. the treatment of osteoporosis and vaginal atrophy. Expert Opin Pharmacother 2009; 10: 2209-20. 2. Cummings SR, et al. PEARL Study Investigators. Lasofoxifene in P epa a ons ...... r r ti ...... postmenopausal women with osteoporosis. N Eng! J Med 2010; 362: 686- ...... 96. Proprietary Preparations (details are given in Volume B) 3. LaCroix AZ, et al. PEARL Investigators. Breast cancer incidence in the randomized PEARL trial of lasofoxifene in postmenopausal osteoporotic Single-ingredient Prepara6ons, Jpn: Bonoteo: Recalbon. women. J Natl Cancer Inst 2010; 102: 1706-15. 4. Ensrud K, et al. Lasofoxifene and cardiovascular events in postmenopausal women with osteoporosis: five-year results from the postmenopausal evaluation and risk reduction with lasofoxifene Neridronate (PEARL) trial. Circulation 2010; 122: 1716-24. 5. Goldstein SR, et al. Postmenopausal evaluation and risk reduction with lasofoxifene (PEARL) trial: 5-year gynecological outcomes. Menopause (r/NN) 2011; 18: 17-22. 6. Peterson GM, et a/. Lasofoxifene: selective estrogen receptor modulator Acide Nerldror\ique; Acido nertdr6nit'o; AciIIJPoHoBaf! Kv.cpota. (6-Amino-l-hydroxyhexylid�ne)diphosphonic acfid. Oxidronate is a bisphosphonate with general properties C.HpNQ.,P2;:277.1 similar to those of the other (p. 1173.3). It Medronate has a strong affinity for bone. A chelate of oxidronate C;l$ = 79778-41-9. disodium with radioactive technetium-99m (p. 2228.1) is UNII �BU27fJ3RIN4. used diagnostically as a bone scanning agent; it is given Medronic Acid {BAN, USAN, piNNJ intravenously. NeridronateSo dium (r/NNM) A<:id rnedronique;Actde Medronlque; Acido medr6n(co; Acidurn medronlcurn; Medrt)nico, acido; Mel!pm;oBaR Natrii . Neridronas: Nerldronate •·· .· · sodico; HaTP11n Hep1-1iJpohaT. UNit -H6:!VB49QOF. Profile Neridronate is an aminobisphdsphonate with Pharmacopoeias. In Bur. (see p. vii). properties to those of the bisphosphonates in general Ph. Eur. 8: (Medronic Add for Radiopharmaceutical (p. 1173.3). It inhibits and is given Preparations). A white or almost white, amorphous or intravenously as the sodium salt in the management of crystalline, hygroscopic powder. Very soluble in water; very osteogenesis imperlecta (p. ll67.3); it has been used in the slightly soluble in absolute alcohol; practically insoluble in treatment of malignant hypercalcaemia (p. 1167.2) and dichlormnethane. Store in airtight containers. Protect from diseases associated with excessive bone turnover such as light. Paget's disease of bone (p. 1169.3) and osteoporosis (p. ll68.l). The intramuscular route has also been used. Medronate Disodium (USAN, piNNMJ References, 1. O'Rourke NP, et al. Treatment of malignant hypercalcaemia with Disodium Medmf)ate (BANIVIJ; Disodiurn Methylene.Dipho­ aminohexane bisphosphonate (neridronate). Br J Cancer 1994; 69: 914- 17. sphonate; MDP; Medronas Dinatticurn; M�dronat� Dis­ odique: Medronato ar 2. Filipponi P, et at. Paget's disease of bone: benefits of neridronate as a first dls6dico; ,£l1<1H p11i'1 Me,!lpaHar. treatment and in cases of relap!>e after dodronate. Bone 1998; 23: 543-8. Disodiurn d.ihydrogen methylenedip�osphonate. 3. Adami S, et al. Short-term intravenous therapy with neridronate in CH4Na,00P2=2200 Paget's disease. Clin Exp Rheumatol 2002; 20: 55-8. 2568 1 -89'4. 4. Adami S, et al. Intravenous neridronate in adults with osteogenesis CAS ,;...:• 18: imperfecta. 1 Bone Miner Res 2003; 126-30. UN)( ....,.· HAY5MT18L3. 5. Braga V, et al. Intravenous intermittent neridronate in the treatment of postmenopausal osteoporosis. Bone 2003; 33: 342-5. 6. Cascella T, et al. Effects of neridronate treatment in elderly women with Profile osteoporosis. J Endocrinol Invest 2005; 28: 202-8. 7. Gatti D, et a!. Intravenous neridronate in children with osteogenesis Medronate is a bisphosphonate with general properties imperfecta: a randomized controlled study. J Bone Miner Res 2005; 20: similar to those of the other bisphosphonates (p. 1173.3 ). It 758-63. 8. Adami S, et al. Intramuscular neridronate in postmenopausal women has a strong affinity for bone. Complexes of medronate with low bone mineral density. Calci[ Tissue Int 2008; 83: 301-7. disodium and stannous chloride or fluoride, or medronic 9. Benucd M, et al. Effects of monthly intramuscular neridronate in acid, stannous chloride dihydrate, and ascorbic acid, are rheumatic patients in chronic treatment with low-dose glucocorticoids. labelled with radioactive technetium-99m (p. 2228.1) and Clin Exp Rheumatol 2009; 27: 567-73. used diagnostically as bone scanning agents; they are given intravenously. Preparations ...... Proprietary Preparations (details are given in Volume B) Hypersensitivity. For reference to a severe allergic reaction attributed to the medronate component of a radiopharma­ Single-ingredient Preparations. Ital.: Nerixia. ceutical, see under Adverse Effects and Precautions of Bis­ phosphonates, p. 1177.1. Odanacatib (USAN, riNNI bdahacarlbllm: OAaHaKaTH6. _ 'Cjianocy�lop;opyl)4f)ooro-4-rnethyl,2-(!i Proprietary Preparations (details are given in Volume B) (25)-N-(1 1 5}c2,2,2" Ph. Eur. 8: (Pamidronate Disodium Pentahydrate). A white trifiuoro-1_-[4' -(rne'!hyl�ulfdny!)(i,1 '-btpherwll-4.'yl]ethyl} · or almost white, crystalline powder. Soluble in water; Single-ingredient Preparations. Denm.: Amerscan Medronatet; amlno)pent� narnipe. practically insoluble in dichloromethane. It is sparingly Irl. : Medronate Draximaget; Israel: Frosstimage Kit (MDP). C2sH21F.l\t,035=525.6 soluble in dilute mineral adds and dissolves in dilute Multi-ingredient Preparations. Denm.: Amerscan Stannoust. C45 -'--' 603139- i9"i alkaline solutions. A 1.0% solution in water has a pH of 7.8 UN/I � N673F6W2 vN. to 8.8.

All cross-references refer to entries in Volume A