Pharmaceutical development of an amorphous solid dispersion formulation of elacridar hydrochloride for proof-of-concept clinical studies

References

• Shukla S, Ohnuma S Ambudkar SV. Improving cancer chemotherapy with modulators of ABC drug transporters. Curr Drug Targets 2011;12:621–30.
   PubMed Web of Science ®Google Scholar
• van Tellingen O, Yetkin-Arik B, de Gooijer MC, et al. Overcoming the blood–brain tumor barrier for effective glioblastoma treatment. Drug Resist Updat 2015;19:1–12.
   PubMed Web of Science ®Google Scholar
• Agarwal S, Sane R, Ohlfest JR, et al. The role of the breast cancer resistance protein (ABCG2) in the distribution of sorafenib to the brain. J Pharmacol Exp Ther 2011;336:223–33.
   PubMed Web of Science ®Google Scholar
• Bihorel S, Camenisch G, Lemaire M, et al. Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar. Pharm Res 2007;24:1720–8.
   PubMed Web of Science ®Google Scholar
• Bihorel S, Camenisch G, Lemaire M, et al. Influence of breast cancer resistance protein (Abcg2) and P-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec) across the mouse blood–brain barrier. J Neurochem 2007;102:1749–57.
   PubMed Web of Science ®Google Scholar
• Breedveld P, Pluim D, Cipriani G, et al. The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res 2005;65:2577–82.
   PubMed Web of Science ®Google Scholar
• Chen Y, Agarwal S, Shaik NM, et al. P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib. J Pharmacol Exp Ther 2009;330:956–63.
   PubMed Web of Science ®Google Scholar
• Tang SC, Nguyen LN, Sparidans RW, et al. Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Int J Cancer 2014;134:1484–94.
   PubMed Web of Science ®Google Scholar
• Durmus S, Sparidans RW, Wagenaar E, et al. Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Mol Pharm 2012;9:3236–45.
   PubMed Web of Science ®Google Scholar
• Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos 2012;40:1612–19.
   PubMed Web of Science ®Google Scholar
• Tang SC, Lankheet NAG, Poller B, et al. P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. J Pharmacol Exp Ther 2012;341:164–73.
   PubMed Web of Science ®Google Scholar
• Malingré MM, Beijnen JH, Rosing H, et al. Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. Br J Cancer 2001;84:42–7.
   PubMed Web of Science ®Google Scholar
• Kruijtzer CMF, Beijnen JH, Rosing H, et al. Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J Clin Oncol 2002;20:2943–50.
   PubMed Web of Science ®Google Scholar
• Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res 2007;13:3276–85.
   PubMed Web of Science ®Google Scholar
• Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci 2013;102:1343–54.
   PubMed Web of Science ®Google Scholar
• Sawicki E, Verheijen RB, Huitema ADR, et al. Clinical pharmacokinetics of an amorphous solid dispersion tablet of elacridar. Drug Deliv Transl Res 2016. [Epub ahead of print]. doi: 10.1007/s13346-016-0346-3.
   PubMedGoogle Scholar
• Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci 1971;60:1281–302.
   PubMed Web of Science ®Google Scholar
• Vo CL, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm 2013;85:799–813.
   PubMed Web of Science ®Google Scholar
• Janssens S, van den Mooter G. Review: physical chemistry of solid dispersions. J Pharm Pharmacol 2009;61:1571–86.
   PubMed Web of Science ®Google Scholar
• He Y, Ho C. Amorphous solid dispersions: utilization and challenges in drug discovery and development. J Pharm Sci 2015;104:3237–58.
   PubMed Web of Science ®Google Scholar
• Shah N, Iyer RM, Mair HJ, et al. Improved human bioavailability of vemurafenib, a practically insoluble drug, using an amorphous polymer-stabilized solid dispersion prepared by a solvent-controlled coprecipitation process. J Pharm Sci 2013;102:967–81.
   PubMed Web of Science ®Google Scholar
• EMA. Stivarga European Public Assessment Report; 2013:1–91. Available from: http://www.ema.europa.eu. [last accessed 24 Aug 2016].
   Google Scholar
• Sharp MJ, Mader CJ, Strachan C. Synthesis of acridine derivative multidrug-resistant inhibitors. Patent number WO98/52923; 1998:1–21.
   Google Scholar
• USP. United States Pharmacopoeia National Formulary Online. Available from: www.usp.org/usp-nf; 2015.
   Google Scholar
• den Brok MWJ, Nuijen B, Lutz C, et al. Pharmaceutical development of a lyophilised dosage form for the investigational anticancer agent Imexon using dimethyl sulfoxide as solubilising and stabilising agent. J Pharm Sci 2005;94:1101–14.
   PubMed Web of Science ®Google Scholar
• Sawicki E, Hillebrand MJ, Rosing H, et al. Validation of a liquid chromatographic method for the pharmaceutical quality control of products containing elacridar. J Pharm Anal 2016;6:268–75.
   Web of Science ®Google Scholar
• FDA. Guidance for industry: dissolution testing of immediate release oral dosage forms; 1997:1–17 [cited 2016 Jul 14]. Available from: http://www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation/guidances/ucm070237.pdf. [last accessed 14 Jul 2016].
   Google Scholar
• Paudel A, Worku ZA, Meeus J, et al. Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations. Int J Pharm 2013;453:253–84.
   PubMed Web of Science ®Google Scholar
• Linn M, Collnot EM, Djuric D, et al. Soluplus® as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo. Eur J Pharm Sci 2012;45:336–43.
   PubMed Web of Science ®Google Scholar
• Alam MA, Ali R, Al-Jenoobi FI, et al. Solid dispersions: a strategy for poorly aqueous soluble drugs and technology updates. Expert Opin Drug Deliv 2012;9:1419–40.
   PubMed Web of Science ®Google Scholar
• Zhang K, Yu H, Luo Q, et al. Increased dissolution and oral absorption of itraconazole/Soluplus extrudate compared with itraconazole nanosuspension. Eur J Pharm Biopharm 2013;85:1285–92.
   PubMed Web of Science ®Google Scholar
• Moes JJ, Koolen SLW, Huitema ADR, et al. Pharmaceutical development and preliminary clinical testing of an oral solid dispersion formulation of docetaxel (ModraDoc001). Int J Pharm 2011;420:244–50.
   PubMed Web of Science ®Google Scholar
• Baghel S, Cathcart H, O’Reilly NJ. Polymeric amorphous solid dispersions: a review of amorphization, crystallization, stabilization, solid-state characterization, and aqueous solubilization of biopharmaceutical classification system class II drugs. J Pharm Sci 2016;105:2527–44.
   PubMed Web of Science ®Google Scholar
• Shah S, Maddineni S, Lu J, et al. Melt extrusion with poorly soluble drugs. Int J Pharm 2013;453:233–52.
   PubMed Web of Science ®Google Scholar
• Bühler V. Application Guide – Kollidon® Polyvinylpyrrolidone excipients for the pharmaceutical industry [Internet]. BasF; 2008:14 [cited 2016 Aug 24]. Available from: https://industries.basf.com.
   Google Scholar
• Lim SM, Pang ZW, Tan HY, et al. Enhancement of docetaxel solubility using binary and ternary solid dispersion systems. Drug Dev Ind Pharm 2015;41:1847–55.
   PubMed Web of Science ®Google Scholar
• Herbrink M, Schellens JHM, Beijnen JH, et al. Inherent formulation issues of kinase inhibitors. J Control Release 2016;239:118–27.
   PubMed Web of Science ®Google Scholar
• ICH. Impurities: guideline for residual solvents Q3C(R5) [Internet]. Int. Conf. Harmon; 2011:1–29 [cited 2016 Nov 6]. Available from: http://www.ich.org/fileadmin/Public_Web_Site/ICH_Products/Guidelines/Quality/Q3C/Step4/Q3C_R5_Step4.pdf. [last accessed 6 Nov 2016].
   Google Scholar
• Tang XC, Pikal MJ. Design of freeze-drying processes for pharmaceuticals: practical advice. Pharm Res 2004;21:191–200.
   PubMed Web of Science ®Google Scholar