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(12) Patent Application Publication (10) Pub. No.: US 2017/0119801 A1 Tabuteau (43) Pub

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(12) Patent Application Publication (10) Pub. No.: US 2017/0119801 A1 Tabuteau (43) Pub US 201701 19801A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2017/0119801 A1 Tabuteau (43) Pub. Date: May 4, 2017 (54) COMPOSITIONS FOR ORAL filed on May 15, 2012, provisional application No. ADMINISTRATION OF ZOLEDRONIC ACID 61/654,292, filed on Jun. 1, 2012, provisional appli OR RELATED COMPOUNDS FOR cation No. 61/654,383, filed on Jun. 1, 2012, provi TREATING COMPLEX REGIONAL PAIN sional application No. 61/655,527, filed on Jun. 5, SYNDROME 2012, provisional application No. 61/655,541, filed on Jun. 5, 2012, provisional application No. 61/764, (71) Applicant: ANTECIP BIOVENTURES II LLC, 563, filed on Feb. 14, 2013, provisional application New York, NY (US) No. 61/762,225, filed on Feb. 7, 2013, provisional application No. 61/767,647, filed on Feb. 21, 2013, (72) Inventor: Herriot Tabuteau, New York, NY (US) provisional application No. 61/767,676, filed on Feb. 21, 2013, provisional application No. 61/803,721, (21) Appl. No.: 15/408,783 filed on Mar. 20, 2013. (22) Filed: Jan. 18, 2017 Publication Classification Related U.S. Application Data (51) Int. Cl. (63) Continuation-in-part of application No. 15/055.386, A63/675 (2006.01) filed on Feb. 26, 2016, which is a continuation of A6II 47/12 (2006.01) application No. 14/635,857, filed on Mar. 2, 2015, A6IR 9/00 (2006.01) now Pat. No. 9,283,239, which is a continuation of (52) U.S. Cl. application No. 14/279,232, filed on May 15, 2014, CPC .......... A61 K3I/675 (2013.01); A61K 9/0053 now Pat. No. 9,149,487, which is a continuation of (2013.01); A61K 47/12 (2013.01); A61 K application No. 14/063,979, filed on Oct. 25, 2013, 47/48038 (2013.01) now Pat. No. 8,802,658, which is a continuation-in part of application No. 13/894,274, filed on May 14, 2013, now abandoned, Continuation-in-part of appli (57) ABSTRACT cation No. 15/347,696, filed on Nov. 9, 2016, which Oral dosage forms of osteoclast inhibitors, such as nitrogen is a continuation-in-part of application No. PCT/ containing bisphosphonates, such as Zoledronic acid in an US2015/032739, filed on May 27, 2015. acid or a salt form, or in a molecular complex can be used (60) Provisional application No. 61/646.538, filed on May to treat or alleviate pain or related conditions, such as 14, 2012, provisional application No. 61/647,478, complex regional pain syndrome. Patent Application Publication May 4, 2017. Sheet 1 of 17 US 2017/01 19801 A1 80. %. 3. 8 . Weice - -8-- - 2ciedronic acid 18 ngin: sq. 8, 2ciedronic acid 20 irgin sq. a .. x - 2ciedronic acid 900 irgin sq. x . 8. s 2 *... * X w -&- ... --8-, 8 130 a . X. - « . x w : 8 -- '. :- - - - -8 3. 80 ----------------------------------------------------------------------------------------------------------------------------------------------------------- Eay lay Day Day Day 2 jay 2 Day 3 lay3 3. (0.5hr) (hi) (3hr) 8. (thr 3. (h) Patent Application Publication May 4, 2017. Sheet 2 of 17 US 2017/01 19801 A1 50% 40% 30% - 20% - 10% Zoecretic Zieroic acid 54 acic: 36 gf gfin Patent Application Publication May 4, 2017. Sheet 3 of 17 US 2017/01 19801 A1 210 - 190 170 - 1so Norna Paw Weice Zoedronic Zoiedric acid 54 mg/m acid 360 mg/m.' Patent Application Publication May 4, 2017. Sheet 4 of 17 US 2017/01 19801 A1 Pair Ecera farth Weight Bearing Patent Application Publication May 4, 2017. Sheet 5 of 17 US 2017/01 19801 A1 left Paw Norra 8 Right Paw Fracture Patent Application Publication May 4, 2017. Sheet 6 of 17 US 2017/01 19801 A1 Weice Zoedronic acid Patent Application Publication May 4, 2017. Sheet 7 of 17 US 2017/01 19801 A1 Weice Zoeiroric acic Patent Application Publication May 4, 2017. Sheet 8 of 17 US 2017/01 19801 A1 Zoiedric acid is diagoed rotate tetrahydrate Patent Application Publication May 4, 2017. Sheet 9 of 17 US 2017/01 19801 A1 38 -8-S8 kg - Bisodigits 2diedraete 88: a . 3. i. Patent Application Publication May 4, 2017. Sheet 10 of 17 US 2017/01 19801 A1 r p s w a was a w Y y . aws was Y * * * * 23. ... f -38 ring Disodiun, Sait A w. A w y & 38 g acid a - 7: rig sodiuin Sait 2008 38 33 38 Congression Force psi} Patent Application Publication May 4, 2017. Sheet 11 of 17 US 2017/0119801 A1 Change in WAS Pain Score Compared to Placebo with Zoiedronic Acid Treatment AFS. Grade (ARS Grade i-2 8 . -8 c. -i. -2. Patent Application Publication May 4, 2017. Sheet 12 of 17 US 2017/0119801 A1 Change in WAS Pain Score Compared to Baseline with Zoiedronic Acid Treatient AKS state ARS racie ARS crities - . -S.8 . Patent Application Publication May 4, 2017. Sheet 13 of 17 US 2017/0119801 A1 Change in WAS Pain Score Compared to Piacebo with Zoiedronic Acic featent at tree vorts Baseine WAS & 5 - A patients Baseine WAS & 33 OAiRS3 gracie 0. afS 3race 8, -2, 8. -8, -8, -2, Patent Application Publication May 4, 2017. Sheet 14 of 17 US 2017/0119801 A1 Change in BM lesion Size Compared to Placebo with Zoiedronic Acid reatient OARS grade OARS Grastie i wa 3. -i. s, -8. Patent Application Publication May 4, 2017. Sheet 15 of 17 US 2017/0119801 A1 was 88;is x3x3x3& acts &streit Siss& Risk: & 88:3 8x8 is 882 3 ise after asciite F. 4 Patent Application Publication May 4, 2017. Sheet 16 of 17 US 2017/0119801 A1 s 3. s s sor Sessie -eeeeeee:3883:38: & &&tyset 8&se:33e &eek. 3 &ees Rises: 8 Beek 8:2:82; Easte G. s. Patent Application Publication May 4, 2017. Sheet 17 of 17 US 2017/0119801 A1 O weeks 4 weeks ise 3etwee fracture at Ora Adsiistratic of aciecirciic Acic US 2017/01 19801 A1 May 4, 2017 COMPOSITIONS FOR ORAL provides an area under the plasma concentration curve of ADMINISTRATION OF ZOLEDRONIC ACID Zoledronic acid of about 4 ngh/mL to about 2000 ngh/mL OR RELATED COMPOUNDS FOR to a human being to which the dosage form is administered. TREATING COMPLEX REGIONAL PAIN 0008. Some embodiments include a dosage form com SYNDROME prising Zoledronic acid in the disodium salt form, wherein the disodium salt form is present in a lower molar amount CROSS-REFERENCE TO RELATED than would be present if the Zoledronic acid were in the APPLICATIONS diacid form; and wherein the Zoledronic acid in the disodium 0001. This application is a continuation-in-part of U.S. salt form has an improved bioavailability as compared to the patent application Ser. No. 15/055.386, filed Feb. 26, 2016, Zoledronic acid in the diacid form to the extent that the lower which is a continuation of U.S. patent application Ser. No. molar amount of the disodium salt in the dosage form does 14/635,857, filed Mar. 2, 2015, now U.S. Pat. No. 9,283,239, not reduce the amount of Zoledronic acid delivered to the which is a continuation of U.S. patent application Ser. No. plasma of a mammal. 14/279,232, filed May 15, 2014, now U.S. Pat. No. 9,149, 0009. Although an oral dosage form with enhanced bio 487, which is a continuation of U.S. patent application Ser. availability with respect to the bisphosphonate compound No. 14/063,979, filed Oct. 25, 2013, now U.S. Pat. No. can be used, the treatment can also be effective using an oral 8,802.658, which is a continuation-in-part of U.S. patent dosage form that includes a bisphosphonate compound, such application Ser. No. 13/894,274, filed May 14, 2013, now as Zoledronic acid, wherein the bioavailability of the bis abandoned, which claims the benefit of U.S. Prov. App. Nos. phosphonate is unenhanced, or is substantially unenhanced. 61/646.538, filed May 14, 2012: 61/647,478, filed May 15, 0010 Some embodiments include a method of relieving 2012: 61/654,292, filed Jun. 1, 2012: 61/654,383, filed Jun. inflammatory pain comprising administering an oral dosage 1, 2012: 61/655,527, filed Jun. 5, 2012: 61/655,541, filed form containing Zoledronic acid to a mammal in need Jun. 5, 2012: 61/764,563, filed Feb. 14, 2013: 61/762,225, thereof, wherein the mammal experiences significant pain filed Feb. 7, 2013: 61/767,647, filed Feb. 21, 2013: 61/767, relief more than 3 hours after administration of the dosage 676, filed Feb. 21, 2013; and 61/803,721, filed Mar. 20, form. 2013; this application is also a continuation-in-part of U.S. 0011. Some embodiments include a method of relieving patent application Ser. No. 15/347,696, filed Nov. 9, 2016, pain associated with an arthritis comprising administering an which is a continuation-in-part of International Pat. App. oral dosage form containing Zoledronic acid to a human No. PCT/US2015/032739, filed May 27, 2015; any of the being in need thereof. applications, U.S. patents issued from, or U.S. publications 0012 Some embodiments include a method of treating of any of the above applications are incorporated by refer complex regional pain syndrome comprising administering ences in their entirety. an oral dosage form containing Zoledronic acid to a mammal in need thereof. SUMMARY 0013 Some embodiments include an oral dosage form comprising Zoledronic acid, wherein the oral bioavailability 0002 Bisphosphonate compounds are potent inhibitors of Zoledronic acid is Substantially unenhanced. For example, of osteoclast activity, and are used clinically to treat bone in some embodiments, the oral bioavailability in the dosage related conditions such as osteoporosis and Paget’s disease form is about 0.01% to about 4%.
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