Table 1. Inhibitors for anaplastic lymphoma kinase (ALK) in or expected to go to clinical trial, 2011.
| Company | Inhibitor | Clinical trial; phase | G/W | Aims of investigation |
|---|---|---|---|---|
| Pfizer | Crizotinib | NCT00932893; III | No | Crizotinib versus standard of care in patients with advanced NSCLC |
| (Xalkori) | NCT01154140; III | No | Randomized, open-label study of the efficacy and safety of crizotinib versus pemetrexed/cisplatin or pemetrexed/carboplatin in previously untreated patients | |
| NCT00939770; I/II | No | Young patients with relapsed or refractory solid tumors, ALCL, CNS, or NBs. | ||
| NCT01121588; I/II | No | Safety and efficacy in patients with tumors except NSCLC that are positive for ALK | ||
| Novartis | NVP-TAE684 | N/A | Not developed | |
| LDK378 | NCT01283516; I | Yes | Safety in ALK-positive/genetically abnormal tumors; no available data. | |
| 3-39 | preclinical | Yes | ||
| Chugai | AF802 (CH5424802) | JapicCTI-101264; I/II | Yes | I. Safety, tolerability, and pharmacokinetic in NSCLC patients with ALK-fusion gene. II. Efficacy and safety of AF802. |
| Infinity | IPI-504* | NCT01228435; II | N/A | Inhibitor of Hsp90, which protects other proteins from being destroyed, possibly also EML4–ALK fusion proteins in NSCLC patients. |
| Astrella | ASP3026 | NCT01284192; I | ND | Safety and tolerability of ASP3026. No preclinical data available but aim for advanced malignancies, B-cell lymphoma, solid tumors, and ALK. |
| Ariad | AP-26113 | preclinical | Yes | AP-26113 abrogates crizotinib-resistant mutations in EML4–ALK. Clinical development 2011 likely. |
| Xcovery | X-396 | preclinical | Yes | X-396 inhibits two ALK point mutations, C1156Y and L1196M, and works in synergy with rapamycin. May initiate clinical trials by the end of 2011. |
| GlaxoSmithKline | GSK-1838705A | preclinical | Yes | Abrogates ALK, and growth of ALCL, some NBs, and a subset of NSCLC. |
*IPI-504 is not an ALK inhibitor, but an Hsp90 inhibitor. ALCL, anaplastic large-cell lymphoma; CNS, central nervous system; EML4, echinoderm microtubule-associated protein-like 4; G/W, ability to inhibit gateway mutation; NB, neuroblastoma, N/A, not applicable; ND, not determined; NSCLC, non-small cell lung cancer.