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| Target (drug previously reported to be in phase 3 trial) | Similar to established targets in combination of A, B, C, and D profiles | Targeted disease conditions | Latest development status (year of report) |
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| CCK-A receptor (dexloxiglumide) | Combination of A, B, C, and D | Irritable bowel syndrome | Positive results in phase III trial (2007) and a large European phase III trial (2010), in talks with FDA for approval (2010) |
|
Coagulation factor IIa
(SR-123781A) | Combination of A, B, C, and D | Venous thromboembolism | Positive results in a large European phase III trial (2008) |
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| NTRK1 (lestaurtinib) | Combination of A, B, C, and D | Acute myeloid leukemia | Lestaurtinib approved by FDA as orphan drug (2006) |
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| 5HT 3 receptor (cilansetron) | Combination of A, C, and D | Irritable bowel syndrome | Positive phase III trial results (2004), filed but withdrawn for FDA approval (2005), still in talks with MHRA and EU (2010) |
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| Heparanase (PI-88) | Combination of A, C, and D | Hepatocellular cancer | PI-88 fast tracked by FDA (2008) |
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| MDR 3 (LY335979) | Combination of A, C, and D | Acute myeloid leukemia | |
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| Orexin receptor (almorexant) | Combination of A, C, and D | Sleep disorders | Positive phase III trial result (2010) |
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Somatostatin receptor 1
(pasireotide) | Combination of A, C, and D | Cushing’s disease, renal cell carcinoma | |
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| NK-2 receptor (saredutant) | Combination of A, C, and D | Depression | Positive phase III trial result (2007), trial discontinued (2009) |
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| BK-2 receptor (icatibant) | Combination of A, B, and C | Hereditary angioedema, traumatic brain injuries | Positive phase III trial results (2006), icatibant approved in EU (2008) |
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| Thrombin receptor (SCH-530348) | Combination of A, B, and C | Cardiovascular disorders | |
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| CXCR4 (plerixafor) | Combination of A, B, and D | Non-Hodgkin’s lymphoma, late-stage solid tumors | Plerixafor approved by FDA (2008) |
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| C1 esterase (Cinryze) | Combination of A, B, and D | Hereditary angioedema | Cinryze approved by FDA (2008) |
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| Sphingosine 1-phosphate receptor 1 (Gilenia) | Combination of A, B, and D | Multiple sclerosis | Positive phase III trial results (2008). FDA granted priority review (2010) |
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| NPYR5 (CGP71683A) | Combination of A, B, and D | Obesity | |
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| Plasma kallikrein (ecallantide) | Combination of A, B, and D | Hereditary angioedema | Positive phase III trial results (2007), ecallantide approved by FDA (2009) |
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