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| THERAPY | RESEARCHER | DESCRIPTION | NAME (if any) | PHASE | REFERENCE | CLINICAL TRIALS (if any) | |
| 1 | EXON SKIPPING USINg ANTISENSE OLIGONUCLEOTIDES (return to top) | ||||||
| A | PMO, morpholino targeting exon 51, | AVI Biopharma, Muntoni F. | Phosphorodiamidate morpholino oligomer targeting exon 51, avi-4658, is well tolerated and restores dystrophin expression in duchenne muscular dystrophy (dmd) boys in a dose dependent manner. | AVI-4568 | Phase ll | AVI BioPharma - News Release | ClinicalTrials.gov Link |
| B | PMO, morpholino targeting exon 45, 50 | AVI Biopharma | Phosphorodiamidate morpholino oligomer targeting exon 45 and 50 | Pre-clinical | AVI BioPharma - News Release | ||
| C | PPMO targeting exon 50 | AVI Biopharma | Peptide conjugated phosphorodiamidate morpholino oligomer targeting exon 50. | AVI - 5038 | Development | AVI news release February 5, 2010 | |
| D | 2-'O-methyl antisense oligos (PS) exon 44 | Prosensa, Aartsma-Rus A. | 2-'O-methyl antisense oligos (PS) targeting exon 44. | PRO044 | Phase ll | J Gene Med. 2009 Mar;11(3):257-66. | ClinicalTrials.gov Link |
| E | 2-'O-methyl antisense oligos (PS) exon 51 | Prosensa, van Deutekom J. | 2-'O-methyl antisense oligos (PS) targeting exon 51. | PRO051 | Phase ll | N Engl J Med. 2007 Dec 27;357(26):2677-86. | ClinicalTrials.gov Link |
| ClinicalTrials.gov Link | |||||||
| F | Guanine Enhanced Exon skipping (6-thioguanine) | Lu QL. | 6-thioguanine enhances morpholino-mediated exon skipping. | Animal | Mol Ther. 2010 Apr;18(4):812-8. | ||
| G | Vivo-morpholinos (vPMOs) | Gene-Tools, Lu QL. | Octa-guanidine conjugated to morpholinos. | Animal | Mol Ther. 2009 May;17(5):864-71. | ||
| H | Exon-skipping Across the Human Dystrophin Gene Transcript | Wilton S., Aartsma-Rus A, Van Ommen G | Skip various exons that aren't now being covered by current trials. | Cell | Mol Ther. 2007 Jul;15(7):1288-96. | ||
| I | Cocktail morpholinos targeting exon 51 | Takeda S. | Cocktail morpholinos targeting exon 51 induced highly efficient dystrophin expression. | Animal | Mol Ther. 2010 Sep 7 | ||
| J | Multiple-skipping ex6/8 | Takeda S., Hoffman E., Partridge TA. | Systemic Exon 6/8 double skipping demosntrated in dystrophic dogs/human cells. | Animal | Ann Neurol. 2009 Jun;65(6):667-76. | ||
| K | Multiple-skipping ex 52/53 | Wilton S. | By-passing the nonsense mutation in the 4 CV mouse model of muscular dystrophy by induced exon skipping. | Animal | J Gene Med. 2009 Jan;11(1):46-56. | ||
| L | 2'-O-Me RNA/ENA chimera ex45/46 | Matsuo M., Sankyo biotech | Induced exon 45 and 46 skipping. | Cell | Nucleic Acids Symp Ser (Oxf). 2004;(48):297-8. | ||
| M | 2'-O-Me RNA/ENA chimera ex 19 | Matsuo M., Sankyo biotech | The exon 19-skipping activity of the RNA/ENA chimera was more than 40 times stronger than that of the corresponding conventional phosphorothioate oligodeoxynucleotide. | Cell | Oligonucleotides. 2004 Spring;14(1):33-40. | ||
| N | Multiple-skipping ex 43/44, 45/51,45-51 | van Deutekom JC. | Double skipping of exon 43 and 44, exon 45 and 51 was achieved. | Cell | Am J Hum Genet. 2004 Jan;74(1):83-92. | ||
| O | Antisense-induced exon skipping for duplications | van Deutekom JC. | The correction of DMD duplications by exon skipping depends on the specific exons targeted. | Cell | BMC Med Genet. 2007 Jul 5;8:43. | ||
| P | Antisense oligonucleotide sequences targeting exon 53 | Dickson G. | 24 AOs of the PMO chemistry designed to target exon 53 of the DMD gene. | Cell | Neuromuscul Disord. 2010 Feb;20(2):102-10. | ||
| Q | Chimeraplast-mediated exon skipping | Bertoni C. | Multiple alternative transcripts were induced by RNA/DNA oligonucleotides (chimeraplasts). | Animal | Hum Mol Genet. 2003 May 15;12(10):1087-99. | ||
| R | Peptide nucleic acid antisense oligonucleotides mediated exon skipping | Wood MJ. | PNA and all PNA-peptide conjugates resulted in significant numbers of dystrophin-positive fibers in the injected tibialis anterior (TA) muscles. | Animal | Mol Ther. 2008 Jan;16(1):38-45. | ||
| S | Muscle targeting peptide Enhanced Exon skipping | Wood MJ. | Muscle-targeting heptapeptide (MSP) fused to an arginine-rich cell-penetrating peptide (B-peptide) and conjugated to a morpholinos | MSP-PMOs | Animal | Hum Mol Genet. 2009 Nov 15;18(22):4405-14. | |
| T | PEG-PEI copolymers | Lutz GJ. | Antisense oligonucleotides complexed with PEG-PEI copolymers. | Animal | Mol Ther. 2006 Jul;14(1):88-96. | ||
| U | Nanopolymers | Lutz GJ. | Improve delivery of exon skipping oligonucleotides and concomitant dystrophin expression in skeletal muscle of mdx mice. | Animal | BMC Biotechnol. 2008 Apr 2;8:35. | ||
| V | Systemic Therapy With Morpholino Oligomers for exon 23 | Dickson G., Partridge TA, Lu QL. | Mdx mice treated for 50 weeks showed a substantial dose-related amelioration of the pathology, | Animal | Mol Ther. 2010 Nov 23 | ||
| particularly in the diaphragm. | |||||||
| W | Systemic Therapy With 2'OMePS for exon 23 | Partridge TA, Lu QL, | Systemic delivery of antisense oligoribonucleotide restores dystrophin expression in body-wide skeletal muscles. | Animal | Proc Natl Acad Sci U S A. 2005 Jan 4;102(1):198-203. | ||
| X | Physiological Characterization of Muscle Strength With Variable Levels of Dystrophin Restoration in mdx Mice Following Local Antisense Therapy for ex23 | Wells D. | A highly significant correlation between the number of dystrophin-positive fibers and resistance to contraction-induced injury. | Animal | Mol Ther. 2010 Oct 5. | ||
| Y | Chimeric Peptide-PMO Conjugate | Wood MJ. | 100% dystrophin-positive fibers and near complete correction of the dystrophin transcript defect in all peripheral muscle groups. Cumulative, enhanced molecular and phenotypic correction. | Animal mdx mice | Mol Ther. 2010 Oct;18(10):1822-9. | ||
| Z | octaguanidine-morpholino oligo conjugate | Widrick JJ | octaguanidine delivery moiety-Morpholino conjugate that targets exon 23 (VMO23), restored function to muscles of mdx mice | VMO 23 | Animal mdx mice | Muscle Nerve. 2011 Oct;44(4):563-70. doi: 10.1002/mus.22126 | |
| AA | antisense oligonucleotide PRO051 | Goemans NM | PRO051 induced detectable, specific exon-51 skipping at doses of 2.0 mg or more per kilogram | systemic PRO051 | Human | N Engl J Med. 2011 Apr 21;364(16):1513-22 | |
| AB | antisense 2'O-methyl oligonucleotides (2'OMePS) and cocktail phosphorodiamidate morpholino oligomers (morpholinos, or PMOs) | Yokota T | multiple exon skipping (double exon skipping) shown here provides the prospect of choosing deletions that optimize the functionality of the truncated dystrophin protein for DMD patients | 2'OMePS,PMO | Animal. Dystrophic phenotype dog | Methods Mol Biol. 2011;709:299-312 | |
| 2 | STOP CODON READ THROUGH (return to top) | ||||||
| A | Ataluren | PTC Therapeutics | Positive trends in muscle function and strength were observed at Week 48 in patients treated with | PTC124 | Phase llb | Nature. 2007 May 3;447(7140):87-91. | ClinicalTrials.gov Link |
| low-dose ataluren | ClinicalTrials.gov Link | ||||||
| B | RTC 13 and RTC14 | Bertoni C. | Determine efficacy of stop codon read through compounds identified by HTS at UCLA | Cell | J Exp Med. 2009 Sep 28;206(10):2285-97. | ||
| C | Gentamicin | Sweeney HL. | After 6 months of gentamicin, dystrophin levels significantly increased.The immunogenic epitope resulting from readthrough | Phase I | J Clin Invest. 1999 Aug;104(4):375-81. | ClinicalTrials.gov Link | |
| D | Negamycin | Matsuda R. | A dipeptide antibiotic restores Dystrophin Expression in Skeletal and Cardiac Muscles of mdx Mice | J Biochem. 2003 Nov;134(5):751-8. | |||
| 3 | Exon Skipping with Gene Transfer (return to top) | ||||||
| A | U7 snRNA Mediated Exon Skipping | Garcia L., Davies KE. | Use adeno-associated viral (AAV) vector containing a modified U7 small nuclear [sn] RNA gene | Animal | Mol Ther. 2009 Jul;17(7):1234-40. | ||
| B | U1 snRNA mediated Exon Skipping | Bozzoni I, Amsterdam Molecular Therapeutics | The gene encoding for the U1 snRNA, a small nuclear RNA involved in the recognition of the 5’-splice site and required for the first step of the splicing reaction, inserted into rAAV. | AMT-080 | Pre-clinical | Proc Natl Acad Sci U S A. 2006 Mar 7;103(10):3758-63 | |
| C | microRNA--miR-31 | Cacchiarelli D | In human DMD myoblasts treated with exon skipping, we demonstrate that miR-31 inhibition increases dystrophin rescue | Human DMD Myoblast | EMBO Rep. 2011 Feb;12(2):136-41 | ||
| 4 | GENE THERAPIES (return to top) | ||||||
| A | Deliver microdystrophin via lentiviral vectors | Kimura E., Chamberlain JS. | Transplantation of primary fibroblasts engineered to express a micro-dystrophin together with a tamoxifen-inducible form of the myogenic regulator MyoD. | Animal | Hum Mol Genet. 2008 Aug 15;17(16):2507-17. | ||
| B | Deliver minidystrophin found in BMD patient or constructed microdystrophin via rAAV | Asklepios Biopharmaceutica | Use a mini dystrophin gene, or microdystrophin with recombinant AAVs. A first clinical trial where patients received local AAV-microdystrophin injections in the arm muscle. | Phase l | J Transl Med. 2007 Sep 24;5:45. | ClinicalTrials.gov Link | |
| C | Delivery of mini-dystrophin in two constructs (Trans-splicing) | Duan D. | One rAAV vector provides the CMV promoter/enhancer region, the second provides the SV40 polyadenylation signal | Animal | Nat Biotechnol. 2005 Nov;23(11):1435-9. | ||
| D | Re-engineered AAV | Samulski/Asklepios | Reengineering the receptor footprints, antigenic and reduced hepatic tropism | Animal | Nat Biotechnol. 2010 Jan;28(1):79-82. | ||
| E | AAV-9 | Xiao X. | Successful transduction in neonatal dog, system wide with immunogenicity | Animal | Molecular Therapy. 2010. Jun;18(8):15011508. | ||
| F | Microutrophin delivery | Chamberlain JS. | Microutrophin delivery through rAAV6 increases lifespan and improves muscle function in dystrophic dystrophin/utrophin-deficient mice | Animal | Mol Ther. 2008 Sep;16(9):1539-45. | ||
| G | Deliver microdystrophin via rAAV | Chamberlain JS., Takeda S., Xiao X., Duan D., Mendell JR. | Restores dystrophin-glycoprotein complex and improves sarcolemma integrity in the mdx | Animal | Circulation. 2003 Sep 30;108(13):1626-32. | ||
| H | Dual High-Capacity Hybrid Viral Vector | De Vries AAF. | Transfer of the Full-Length Dystrophin-Coding Sequence into Muscle Cells by a Dual High-Capacity Hybrid Viral Vector with Site-Specific Integration Ability | Animal | J Virol. 2005 Mar;79(5):3146-62. | ||
| I | ultrasound and microbubble mediated in vivo gene transfer. | Petrof BJ., Wells D., Partridge TA. | antisense oligonucleotides or gene transfer using ultrasound and microbubble | Animal | Mol Ther. 2002 Nov;6(5):687-93. | ||
| J | Hybrid vector system | Duan D. | A hybrid vector system expands adeno-associated viral vector packaging capacity in a transgene-independent manner. | Animal | Mol Ther. 2008 Jan;16(1):124-30. | ||
| K | Chimeraplast-mediated gene correction | Bertoni C. | Mutation correction by RNA/DNA oligonucleotides (chimeraplasts) | Animal | Hum Mol Genet. 2003 May 15;12(10):1087-99. | ||
| L | Dystrophin Immunity in Duchenne’s | Mendell JR. | Dystrophin-specific T cells were detected after treatment with rAAV. | Human | N Engl J Med. 2010 Oct 7;363(15):1429-37. | ||
| Muscular Dystrophy | |||||||
| M | Exon Exchange Approach | Garcia L. | Minigene was cotransfected with a variety of exon exchange constructions, differing in their annealing domains. | Animal MDX mice | PLoS One 2010 5:e10894 | ||
| N | Human artificial chromosomes (HACs) | Kazuki Y | Succeeded in complete correction of a genetic deficiency in iPS cells derived from a human Duchenne muscular dystrophy patient using the HAC technology | Cell. iPS cells derived from a human Duchenne muscular dystrophy | Nihon Rinsho. 2011 Dec;69(12):2142-7 | ||
| O | 8K-NBD peptide treatment to AAV9 minidystrophin gene | Reay DP | Increased levels of recombinant dystrophin expression suggesting that 8K-NBD treatment promoted an environment in muscle tissue conducive to higher levels of expression | 8K-NBD & AAV9 | Animal mdx mice | Mol Med. 2012 Jan 5. doi: 10.2119/molmed.2011.00404 | |
| P | Translational Optimized AAV Vector | Bowles DE | AAV2.5 vector was safe and well tolerated, lays the foundation of customizing AAV vectors that best suit the clinical objective | AAV2.5 | Phase 1 | Mol Ther. 2011 Nov 8. doi: 10.1038/mt.2011.237 | |
| 5 | CELL THERAPIES (return to top) | ||||||
| A | Myoblast Transplantation | Tremblay JP. | Transplant myogenic precursors from healthy donors. | Phase IA | Mol Ther. 2009 Jul;17(7):1122-4. | ||
| B | Mesoangioblast transplantation | Cossu G. | Myogenic cells derived from bone marrow grafts delivered to produce widespread skeletal muscle via distribution through the vasculature. | Phase I (3 patients) | Nature. 2006 Nov 30;444(7119):574-9., | Cure Duchenne Founders Blog | |
| C | Transplantation of exon-skipping-engineered patient stem cells | Torrente Y and Garcia L. | lentiviral vectors expressing antisense oligonucleotides in order to induce an efficient exon skipping of CD133+ stem cells. | Animal | Cell Stem Cell. 2007 Dec 13;1(6):646-57. | ||
| D | Hematopoietic cell transplantation | Storb R. | Intramuscular injection of freshly isolated muscle-derived cells from the HCT donor into dog recipients. | Animal | Mol Ther. 2008 Jul;16(7):1340-6. | ||
| E | Embryonic Stem Cells | Perlingeiro RCR. | Functional skeletal muscle regeneration from differentiating embryonic stem cells. | Animal | Nat Med. 2008 Feb;14(2):134-43. | ||
| F | Cord Blood Cells | Zatz M. | Stem cells from umbilical cord blood differentiate into myotubes and express dystrophin in vitro | Cell | Biol Cell. 2007 Apr;99(4):185-96. | ||
| G | Muscle-derived stem cells | Huard J. | Transplanted MDSCs generated | Animal | Gene Ther. 2005 Aug;12(16):1264-74. | ||
| large grafts consisting primarily of numerous dystrophin positive | |||||||
| myocytes in mdx heart. | |||||||
| H | iPS cells | Heike T., Oshimura M. | iPS cells have the potential to be used in clinical treatment of muscular dystrophies. | Animal | Mol Ther. 2010 Feb;18(2):386-93. | ||
| I | Bone marrow stromal cells | Dezawa M. | Inducing skeletal muscle lineage cells from human and rat general adherent MSCs with an efficiency of 89%. | Animal | Science. 2005 Jul 8;309(5732):314-7. | ||
| J | MGMT (P140K)-mediated enrichment strategy | Gunning PW, Hardeman EC. | Adult stem cells are given a gene that makes them resistant to chemotherapy, which is used to clean out damaged cells and allow the new stem cells to take hold. | Animal | Stem Cells. 2009 May;27(5):1098-108. | ||
| K | Placental artery-derived endothelial (hPAE) cells | Umezawa A. | hPAE cells conferred dystrophin to myocytes of the 'immunocompetent' mdx mice with extremely high efficiency. | Animal | Hum Mol Genet. 2010 Nov 8. | ||
| L | Menstrual blood-derived cells | Umezawa A. | Menstrual blood-derived cells confer human dystrophin expression in the murine model of Duchenne muscular dystrophy. | Animal | Mol Biol Cell. 2007 May;18(5):1586-94. | ||
| M | Placenta-derived cells | Umezawa A. | In vivo implantation of placenta-derived cells into dystrophic muscles of immunodeficient mdx mice restored sarcolemmal expression of human dystrophin. | Animal | J Cell Physiol. 2010 Jun;223(3):695-702. | ||
| N | Blocking the Myostatin Signal With a Dominant Negative Receptor Improves the Success of Human Myoblast Transplantation | Tremblay JP. | Blocking the Myostatin Signal With a Dominant Negative Receptor Improves the Success of Human Myoblast Transplantation in Dystrophic Mice. | lentivirus pCMV-dnActRIIB; folistatin | Animal mdx mice | Mol Ther. 2010 Aug 10. | |
| O | Hematopoietic prostaglandin d synthase inhibitors | Kamauchi S | Oral administration of HQL-79 markedly suppressed prostaglandin D production, reduced necrotic muscle volume, and improved muscle strength in mdx dystrophic mice | HQL-79 | Animal mdx mice | Brain Nerve. 2011 Nov;63(11):1261-9 | |
| P | Human Adipose-Derived Mesenchymal Stromal cells | Vieira NM | GRMD dogs without immunosuppression are able to reach the host muscle and express human dystrophin | hASCs systemically | Animal GRMD Dogs | Cell Transplant. 2011 Oct 14 | |
| Q | human artificial chromosomes (HACs) | Tedesco FS | Stem cell-mediated transfer of a human artificial chromosome ameliorates muscular dystrophy | HAC Vector Genetically corrected mesoangioblast. | Animal mdx mice | Sci Transl Med. 2011 Aug 17;3(96):96ra78 | |
| 6 | UTROPHIN UPREGULATION/HDAC INHIBITION (return to top) | ||||||
| A | A small molecule utrophin up-regulator BMN 195 | BioMarin | BMN 195 Program Discontinued due to Pharmaceutical and Pharmacokinetic Challenges. Handed back to Summit. See Summit 1100. | BMN 195 | Phase I | BioMarin News release August 2, 2010 | |
| B | TAT Utrophin | Ervasti J. | Utrophin (Utr) or DeltaR4-21 "micro" utrophin (muUtr) protein modified with the cell-penetrating TAT protein transduction domain. | Animal | PLoS Med. 2009 May 26;6(5):e1000083. | ||
| C | Heregulin | Khurana TJ. | Heregulin ameliorates the dystrophic phenotype in mdx mice with utrophin upregulation. | Animal | Proc Natl Acad Sci U S A. 2004 Sep 21;101(38):13856-60. | ||
| D | Valproic acid | Kaufman SJ. | Activated PI3/AKT/mTOR pathway and Ameliorates Pathology in a Mouse Model. | Animal | Am J Pathol. 2009 Mar;174(3):999-1008. | ||
| E | L-arginine | de la Porte S. | Utrophin upregulation via NO and HDAC pathways. | Animal | Neurobiol Dis. 2005 Oct;20(1):123-30. | ||
| F | GW501516 | Jasmin BJ. | PPARbeta/delta agonist stimulates utrophin A expression in skeletal muscle fibers. | Animal | Hum Mol Genet. 2009 Dec 1;18(23):4640-9. | ||
| G | IL6 | Takeda S. | Interleukin 6 induces overexpression of the sarcolemmal utrophin in neonatal mdx skeletal muscle. | Animal | Hum Gene Ther. 2002 Mar 1;13(4):509-18. | ||
| H | A small molecule utrophin up-regulator SMT C1100 | Summit plc, Davies KE. | Summit plc and Davies are continuing with BM195 (now C1100) and working on reformulated follow up compounds | C1100 | Phase I -reformulated compound | Summit News Release | |
| 7 | MYOSTATIN INHIBITION (return to top) | ||||||
| A | Anti myostatin antibody | Wyeth Pharmaceuticals, WagnerKR., Khurana TS. | Announced it will not continue development of MYO-029 for muscular dystrophy. | MYO-029 Stamulumab | Phase I/ll | Nature. 2002 Nov 28;420(6914):418-21. | |
| B | Myostatin inhibitor | Acceleron Pharma | Soluble activin receptor type IIB or ActRIIB | ACE-031 | Phase ll | Acceleron Pharma News Release May 5, 2010 | ClinicalTrials.gov Link |
| C | rAAV to overexpress a secretable dominant negative myostatin | Sweeney HL. | Systemic myostatin inhibition via liver-targeted gene transfer in normal and dystrophic mice. | Animal | PLoS One. 2010 Feb 11;5(2):e9176. | ||
| D | AAV delivery of follistatin | Mendell JR. | Alternatively spliced cDNA of follistatin (FS344) delivered by adeno-associated virus (AAV) to muscle. | Animal | Muscle Nerve. 2009 Mar;39(3):283-96. | ||
| E | Myostatin propeptide gene delivery | Xiao X. | Myostatin propeptide gene delivery by adeno-associated virus serotype 8 vectors enhances muscle growth and ameliorates dystrophic phenotypes in mdx mice. | Animal | Muscle Nerve. 2009 Mar;39(3):283-96. | ||
| F | Propeptide systemic delivery via RAAV8 vector | Foster K. | Intravenous Transfer of Myostatin Propeptide Leads to Systemic Functional Improvements of Slow but Not Fast Muscle. | Animal | Rejuvenation Res. 2009 Apr;12(2):85-94. | ||
| G | Systemic follistatin via AAV type 1 vector | Kaspar B. | AAV1-FS344 injected into the quadriceps induced pronounced and durable increases in muscle size and strength in monkey. | Animal | Sci Transl Med. 2009 Nov 11;1(6):6ra15. | ||
| H | Follistatin induction via Histone deacetlyase inhibitors | Puri PL., Sartorelli V. | Deacetylase Inhibitors Increase Muscle Cell Size by Promoting Myoblast Recruitment and Fusion through Induction of Follistatin. | Animal | Dev Cell. 2004 May;6(5):673-84. | ||
| I | Follistatin induction via nitric oxide | Clementi E., Cossu G. | NO and cGMP induce expression of follistatin, and this secreted protein mediates their action in myogenesis. | Animal | J Cell Biol. 2006 Jan 16;172(2):233-44. | ||
| J | Recombinant myostatin antagonist | Salerno S. | Short-term blockade of myostatin, through stage-specific administration of a myostatin antagonist, significantly enhanced muscle regeneration. | Myst-Ant1,2,3 | Animal | Mol Ther. 2007 Aug;15(8):1463-70. | |
| K | FS I-I | Tsuchida K. | Myostatin inhibition by a follistatin-derived peptide ameliorates the pathophysiology of muscular dystrophy model mice. | Animal | Acta Myol. 2008 Jul;27:14-8. | ||
| L | Myostatin Exon Skipping | Dickson G. | Antisense-induced Myostatin Exon Skipping Leads to Muscle Hypertrophy in Mice Following Octa guanidine Morpholino Oligomer Treatment. | Animal | Mol Ther. 2010 Oct 5. | ||
| 8 | TGFβ Inhibition/Anti-Fibrosis (return to top) | ||||||
| A | Losartan | Dietz HC. | Selective competitive angiotensin II receptor type 1 receptor antagonist, down regulates expression of TGF-beta. | Cozaar | Animal | Nat Med. 2007 Feb;13(2):204-10. | |
| B | Imatinib mesilate | Costa MC., Zhou L. | TGF Blocker. Improves regeneration after injury. | Gleevec, Imatinib | Animal | J Neuroimmunol. 2009 Jul 25;212(1-2):93-101. | |
| C | Suramin | Huard J. | TGF-β1 blocker. Antifibrotic effects in injured skeletal muscle after laceration. | Germanin | Animal | J Appl Physiol. 2003 Aug;95(2):771-80. | |
| D | Halofuginone | Anderson JE. | Blocks TGFβ-mediated collagen synthesis. | Pre-clinical | Am J Physiol Heart Circ Physiol. 2008 Apr;294(4):H1550-61. | Halotherapeutics News | |
| E | Pirfenidone | Hoey AJ | TGF-beta antagonist, pirfenidone, reduces cardiac fibrosis. | Animal | Muscle Nerve. 2006 Sep;34(3):327-34. | ||
| F | Formoterol | Lynch G. | Beta(2)-adrenoceptor agonist (beta(2)-agonist) improves muscle function in dystrophic mdx mice. | Animal | Neuromuscul Disord. 2007 Jan;17(1):47-55. | ||
| G | Osteopontin | Miceli C., Spencer M., Hoffman E. | Thought to promote fibrosis, elevated levels found in humans w/ DMD. continue to evaluate osteopontin as a therapeutic target for DMD. | Animal | J Clin Invest. 2009 Jun;119(6):1583-94. | ||
| H | Tamoxifen | Vainzof M. | Estrogen receptor modulator. act on TGF-beta.Tamoxifen increases muscular strength of the mdx dystrophic mice. | Animal | Abstracts from 10th International Congress of World Muscle Society | ||
| I | Bowman-Birk inhibitor concentrate (BBIC) | Sweeney HL. | BBIC treatment increases mass and strength, while decreasing fibrosis in skeletal muscles of the mdx mouse. | Animal | J Appl Physiol. 2010 Nov;109(5):1492-9. | ||
| J | Activin IIB receptor blockade | Sweeney HL. | Systemic inhibition of activin IIB receptor signaling via adeno-associated virus (AAV)-mediated gene transfer | Animal | Muscle Nerve. 2010 Nov;42(5):722-30. | ||
| K | BMP antagonists | 't Hoen PA. | BMP antagonists enhance myogenic differentiation and ameliorate the dystrophic phenotype in a DMD mouse model. | Noggin, dorsomorphin and LDN-193189 | Animal | Neurobiol Dis. 2011 Feb;41(2):353-60. | |
| 9 | NF-kB inhibition/anti inflammatory (return to top) | ||||||
| A | Flavocoxid | Messina S., Vita G. | Anti-inflammatory, anti-oxidant and NF-kB inhibition properties. | Animal | Exp Neurol. 2009 Dec;220(2):349-58. | ||
| B | Curcumin | Zhu MS | NF-kB inhintor, it improved sarcolemmic integrity and enhanced muscle strength after intraperitoneal (i.p.) injection. | Animal | Mol Cells. 2008 Jun 30;25(4):531-7. | ||
| C | UDCA | Carlson CG. | Treatment with inhibitors of the NF-κB pathway improves whole body tension development in the mdx mouse. | Animal | Neuromuscul Disord. 2009 Feb;19(2):131-9. | ||
| D | NBD (Nuclear factor-kappa B inhibitory peptide) | Kumar A | Matrix metalloproteinase-9 inhibition ameliorates pathogenesis and improves skeletal muscle regeneration in muscular dystrophy. | Animal | Hum Mol Genet. 2009 Jul 15;18(14):2584-98. | ||
| E | NFκB/NBD peptides , (pyrollidine dithiocarbamate, PDTC) | Siegel A. | Chronic treatment with agents that stabilize cytosolic IkappaB-alpha enhances survival and improves resting membrane potential in mdx. | Animal | Neurobiol Dis. 2005 Dec;20(3):719-30 | ||
| F | HQL-79 | Urade Y | Prostaglandin (D)2 synthase inhibitor suppresses Muscular Necrosis. | Animal | Am J Pathol. 2009 May;174(5):1735-44. | ||
| G | Tβ4 | RegeneRx, Spurney C., Nagaraju K. | Naturally occurring peptide, downregulates inflam cytokines and NF-kB, upregulates AkT surival kinases, Regulates F and G actins. | Thymosim Beta 4 | Animal | PLoS One. 2010 Jan 29;5(1):e8976. | |
| H | Cromolyn | Neto HS, Pollina C., Grounds MD. | Mast cell stabilizer, Disodium cromoglycate protects dystrophin-deficient muscle fibers from leakiness. | Animal | Muscle Nerve. 2008 Jan;37(1):61-7. | ||
| I | L-Arginine | Mornet D. | L-Arginine Decreases Inflammation and Modulates the Nuclear Factor-{kappa}B/Matrix Metalloproteinase Cascade in Mdx Muscle Fibers. | Animal | Am J Pathol. 2008 Jun;172(6):1509-19. | ||
| J | Arginine butyrate | Nagaraju K., Faust Pharmaceuticals | Arginine butyrate treatment improved grip strength and decreased fibrosis in the gastrocnemius muscle. | FP0023 | Animal | PLoS One. 2010 Jun 21;5(6):e11220. | |
| K | Haelan 951/BBIC | Tseng BS. Sweeney L., Walter G., Vandenbourne K. | Protease inihibitor, Anti-inflammatory, neuroprotection? | Cell | FASEB J. 2009 Oct;23(10):3325-34. | ||
| L | Inhibition of the IKK/NF-kappaB pathway by AAV gene transfer | Wang B. | Inhibition of IKKα or IKKβ in dystrophic muscle reduces the adverse effects of NF-κB signaling. | Animal | Gene Ther. 2010 Dec;17(12):1476-83. | ||
| 10 | TNF-alpha inhibition (return to top) | ||||||
| A | BKT-104 (oral TNF alpha inhibitor) | Carvalho AAS, Feder D. | A small molecule which has potent anti-inflammatory properties. | Animal | Annual Meeting of American Academy of Neurology, 2009 | ||
| B | cV1q | Grounds MD. | Anti TNF-alpha monoclonal (Centocor) Reduced muscle necrosis and long-term benefits in dystrophic mdx mice. | Animal | Neuromuscul Disord. 2008 Mar;18(3):227-38. | ||
| C | LMP-420 | Bizario J. | LMP-420 treated mice showed significantly-decreased CK levels and amelioration of muscular degeneration. | Animal | Presentation at NIDB 2008 (PDF) | ||
| D | Etanercept | De Luca A. | Pharmacological approaches to oxidative stress and altered calcium homeostasis in fxl impairment and degenreation. | Animal | Neuropathol Appl Neurobiol. 2007 Jun;33(3):344-59. | ||
| 11 | Anti-Oxidants (return to top) | ||||||
| A | Green Tea Extract | Ruegg U, Stoward PJ. | Antioxidant Green tea extract decreases muscle necrosis in mdx mice and protects against reactive oxygen species. | Phase ll | Am J Clin Nutr. 2002 Apr;75(4):749-53. | ||
| B | Coenzyme Q10 | Simonsen R. | Restore cellular creatinine stores (regulate cellular energy and protein turnover). | Phase ll | Biochim Biophys Acta. 1995 May 24;1271(1):281-6. | ClinicalTrials.gov Link | |
| C | Melatonin | Ruegg T., Acuña-Castroviejo D. | Anti-oxidant Melatonin prevents oxidative stress-mediated mitochondrial permeability transition and death in skeletal muscle cells. | Clinical | J Pineal Res. 2010 Apr;48(3):282-9. | ||
| D | N-Acetylcysteine | Allen DG. | N-acetylcysteine (NAC) provided protection against dystrophic muscle damage in the mdx mouse. | Animal | J Physiol. 2008 Apr 1;586(7):2003-14 | ||
| E | Catena/Idebenone/Sovrima® | Santhera Pharmaceuticals | Small molecule optimized to facilitate the transport of electrons within mitochondria, which is necessary for the production of cellular energy. It is a synthetic analogue of ubiquinone and is a potent antioxidant. | Phase lll | Santhera Pharmaceuticals presentation | ClinicalTrials.gov Link | |
| ClinicalTrials.gov Link | |||||||
| F | (Epigallocatechin-3-Gallate (EGCG) | Ruegg UT. | Green tea extract and its major polyphenol ()-epigallocatechin gallate improve muscle function in a mouse model for Duchenne muscular dystrophy. | Animal | Am J Physiol Cell Physiol. 2006 Feb;290(2):C616-25. | ClinicalTrials.gov Link | |
| G | Alpha-lipoic acid/l-carnitine | Mornet D. | Treatment decreased the plasmatic creatine kinase level, the antioxidant enzyme activity, and lipid peroxidation products in mdx diaphragm. | Animal | Am J Pathol. 2007 Feb;170(2):633-43. | ||
| H | BN 82270 | De Luca A. | A novel chimeric compound dually acting as calpain inhibitor and anti-oxidant. | Animal | Neuromuscul Disord. 2006 Apr;16(4):237-48. | ||
| I | Glutamine | Mok E., Hankard R. | Delay protein breakdown. l-Glutamine administration reduces oxidized glutathione and MAP kinase signaling in dystrophic muscle of mdx mice. | Phase III | Pediatr Res. 2008 Mar;63(3):268-73. | ||
| J | Pargyline, an MAO inhibitor | Canton M. | Pargyline, an MAO inhibitor, reduced ROS accumulation along with a beneficial effect on the dystrophic phenotype. | Animal | Hum Mol Genet. 2010 Nov 1;19(21):4207-15. | ||
| 12 | IGF-1 (return to top) | ||||||
| A | IGF-1 analogue (LR-IGF-1) | Lynch GS., Rutter M. | Insulin-like growth factor-I analogue protects muscles of dystrophic mdx mice from contraction-mediated damage. | Animal | Exp Physiol. 2008 Nov;93(11):1190-8. | ||
| B | Glucose regulated protein 94 | Barton ER, Argon Y. | GRP94 may be a new therapeutic target to boost IGF-1. | Animal | Biochim Biophys Acta. 2010 Feb;1803(2):333-41. | ||
| C | Igf1 codelivery with rAAV/microdystrophin | Chamberlain JS. | Phenotypic improvement of dystrophic muscles by rAAV/microdystrophin vectors is augmented by Igf1 codelivery. | Animal | Mol Ther. 2005 Sep;12(3):441-50. | ||
| D | Increlex - (mecasermin (rDNA origin) injection) | Ipsen Inc. | replacement for IGF-1 | Increlex | Ph 1 Pilot Study | Safety and Efficacy Study of IGF-1 in Duchenne Muscular Dystrophy - Full Text View - ClinicalTrials.gov | |
| 13 | α7-integrin upregulation (return to top) | ||||||
| A | Laminin 111 | Burkin DJ., Prothelia, Inc. | Increases α7-integrin expression. Laminin-111 protein therapy prevents muscle disease in the mdx mouse model for Duchenne muscular dystrophy. | Animal mdx mice | Proc Natl Acad Sci U S A. 2009 May 12;106(19):7991-6. | Prothelia - Pipeline | |
| B | α7-integrin regulation | Kaufman SJ. | Increasing {alpha}7β1-integrin promotes muscle cell proliferation, adhesion, and resistance to apoptosis without changing gene expression. | Animal | Am J Physiol Cell Physiol. 2008 Feb;294(2):C627-40. | ||
| C | Laminin-111 | Gawlik KI | Transgenic expression of Laminin α1 chain does not prevent muscle disease in the mdx mouse model for Duchenne muscular dystrophy. | laminin 111 | Animal mdx, mdxLM alpha 1 mice | Am J Pathol. 2011 Apr;178(4):1728-37 | |
| 14 | nNOS pathway enhancement (return to top) | ||||||
| A | PDE5 inhibition | Des Rosiers C., Wagner KR., Campbell KP., Beavo JA., Asakura A. | Regulate excitation-contraction coupling and vasodilatation and glucose uptake during exercise. Role in muscle repair and regeneration.Sildenafil has been shown to delay and even prevent heart failure in the DMD animal model. | Revatio, sildenafil citrate (Viagra) | Phase ll | Proc Natl Acad Sci U S A. 2008 May 13;105(19):7028-33. | ClinicalTrials.gov Link |
| B | PDE5 inhibition | Yasuhara SE. | The vasoactive drug tadalafil, a phosphodiesterase 5 inhibitor, administered to mdx mice ameliorated muscle damage. | Tadalafil (Cialis) | Animal | PLoS One. 2007 Aug 29;2(8):e806. | ClinicalTrials.gov Link |
| C | nNOS upregulator | Clementi E. | a nitric oxide-releasing derivative of flurbiprofen. | HCT 1026 | Animal | Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):264-9. | |
| 15 | Angiotensin-converting enzyme (ACE) inhibitor/ beta-blocker for cardiomyopathy management (return to top) | ||||||
| A | Angiotensin-converting enzyme (ACE) inhibitor | Scott WA. | Angiotensin-converting enzyme inhibitors in the management of cardiomyopathy. 10 of 26 patients (43%) with Duchenne muscular dystrophy responded to the use of enalapril. | Enalapril | Clinical | Am J Cardiol. 2006 Sep 15;98(6):825-7 | ClinicalTrials.gov Link |
| B | Beta-blocker | Nakanishi T. | Beta-blocker medication is known to improve the prognosis of chronic heart failure of adults. | Carvedilol | Phase lV | Circ J. 2006 Aug;70(8):991-4. | ClinicalTrials.gov Link |
| C | A study to combat heart disease in muscular dystrophy | Mendell JR. | Improve cardiac care by establishing the best medication regimen and to look at the best time to start treatment to protect the patient from heart failure. | Clinical | News release from Nationwide Hospital 7/14/2009 | ||
| D | ACE receptor blocker | Fakhfakh R | Losartan enhances the success of myoblast transplantation | losartan | Dystrophic mice | Cell Transplant. 2011 Apr 29 | |
| 16 | Corticosteroid (return to top) | ||||||
| A | Prednisone | Myer E. | A useful palliative treatment. | Clinical | Lancet. 1974 Dec 14;2(7894):1409-12. | ||
| B | Deflazacort | Flores D. | DF appears as an alternative to prednisone preserving its benefits but with fewer side-effects. | Calcort in UK | Clinical | Neuromuscul Disord. 1991;1(4):261-6. | |
| C | Long-circulating prednisolone liposomes. | Weller C | Liposomal encapsulation is not superior in treatment efficacy compared with conventional prednisolone In improving Motor performance of young dystrophic mdx mice | polyethylene-glycol-coated liposomes encapsulating prednisolone was compared with free prednisolone | Animal mdx mice | J Neurosci Res. 2012 Jan 18. doi: 10.1002/jnr.22825 | |
| 17 | Other (return to top) | ||||||
| A | IL-15 | Lynch GS. | Anabolic cytokine Interleukin-15 administration improves diaphragm muscle pathology and function in dystrophic mdx mice. | Animal | Am J Pathol. 2005 Apr;166(4):1131-41. | ||
| B | Albuterol | Lynch GS. | Low dose beta(2)-adrenoceptor agonist administration improves muscle function in dystrophic mdx mice without increasing fatigue. | Salbutamol | Animal | Neuromuscul Disord. 2007 Jan;17(1):47-55. | |
| C | Velcade and MLN273 | Lisanti MP. | Blocking proteosome. blocks the degradation of dystrophin and dystrophin-associated proteins in mdx mice. | Animal | Cell Cycle. 2007 May 15;6(10):1242-8. | ||
| D | Human Growth Hormone (HGH) | Politano L.. | Induces a hypertrophic response associated with a significant reduction of brain natriuretic peptide plasma levels and a slight improvement of systolic function. | Clinical | Eur Heart J. 2003 Apr;24(7):664-72. | ||
| E | Methazolamide or dichlorphenamide | Segalat L. | Carbonic anhydrase inhibitors. C. elegans-based screen coupled with a mouse model validation strategy. | Animal | Hum Mol Genet. 2009 Nov 1;18(21):4089-101. | ||
| F | MG-132 | Lisanti MP. | Proteasome Inhibitor (MG-132) Treatment of mdx Mice Rescues the Expression and Membrane Localization of Dystrophin and Dystrophin-Associated Proteins. | Animal | Cell Cycle. 2007 May 15;6(10):1242-8. | ||
| G | PG-873637 | Isfort RJ. | Corticortopin releasing factor 2 receptor agonist treatment significantly slows disease progression in mdx mice. | Animal | BMC Med. 2007 Jul 12;5:18. | ||
| H | GsMTx4 | Sachs F., Allen DG. | Streptomycin and the spider venom toxin GsMTx4, prevented the rise of resting [Ca2+]i and partially prevented the decline of tetanic [Ca2+]i and force. | Cell | J Physiol. 2005 Jan 15;562(Pt 2):367-80. | ||
| I | Debio 025/ CypD/ CsA | Molkentin JD., Ruegg UT., Bernardi P. | Cyclophilin D Inhibitor; anti-apoptotic properties. as, effective as or slightly better than, prednisone in mitigating muscular dystrophy in the mdx mouse. | Animal | Neuromuscul Disord. 2010 Jul 14. | ||
| J | Creatine Monohydrate | Tarnopolsky MA. | Nutritional therapy improves function and complements corticosteroid intervention in mdx mice. | Phase III | Muscle Nerve. 2006 Jan;33(1):66-77. | ||
| K | PAMH (Pyridine Activator of muscle cell hypertrophy) | Olson EN. | Potential target for muscle growth. | Animal | Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2870-5. | ||
| L | Membrane sealant poloxamer 188 | Metzger JM., Phrixus Pharmaceuticals | In vivo administration of poloxamer 188 to dystrophic mice instantly improved ventricular geometry and blocked the development of acute cardiac failure. | P-188 | Pre-Clinical | J Clin Invest. 2010 Apr 1;120(4):1140-50. | Phrixus News |
| M | TRPV2 | Iwata Y. | Dominant-negative inhibition of Ca2+ influx via TRPV2 ameliorates muscular dystrophy in animal models. | Animal | Hum Mol Genet. 2009 Mar 1;18(5):824-34. | ||
| N | Far Infrared Radiation | Nedd K. | Far Infrared radiation for 30 to 40 minutes per treatment session. | Phase I | Clinical Trial database | ClinicalTrials.gov Link | |
| O | GLPG0492 | Galapagos NV. | Orally available small molecule that Galapagos has developed in its Selective Androgen Receptor Modulator (SARM) program. | pre-clinical | Galapagos News Release, May 20, 2010 | ||
| P | Biglycan | Fallon JR. | Biglycan regulates the expression and sarcolemmal localization of dystrobrevin, syntrophin, and nNOS. | Pre-Clinical | FASEB J. 2006 Aug;20(10):1724-6. | Tivorsan.com Link | |
| Q | Flt-1 gene knockout | Asakura A. | Increasing the vasculature in DMD may ameliorate the histological and functional phenotypes associated with this disease. | Mdx mice Crossed with Flt-1 gene knockout mice | Animal. Mdx mice & Flt-1 gene knockout mice | Hum Mol Genet. 2010 Nov 1;19(21):4145-59. | |
| R | transduction of full-length dystrophin | Ishizaki M | Rescue from respiratory dysfunction by transduction of full-length dystrophin to diaphragm via the peritoneal cavity in utrophin/dystrophin double knockout mice | intraperitoneal injection of a helper-dependent adenovirus vector (HDAdv) containing the full-length dystrophin expression cassett | Animal dko mice | Mol Ther. 2011 Jul;19(7):1230-5. doi: 10.1038/mt.2011.58 | |
| S | Histone deacetylase inhibitors | Consalvi S | The ability of HDACi to counter the progression of muscular dystrophies points to HDACs as a crucial link between specific genetic mutations and downstream determinants of disease progression | suberoylanilide hydroxamic acid (SAHA) and ITF2357 (givinostat) | Animal mdx mice | Mol Med. 2011 May-Jun;17(5-6):457-65. doi: 10.2119/molmed.2011.00049 | |

