There is an abstract for X-396 that included 30 patients (21 NSCLC and only 13 ALK+). Maximum tolerated dose not reached. Current maximum dosage was 250mg.
In the 6 ALK+ patients who received greater than or equal to 200mg, 82% had a partial response (greater than 30%) and 17% had stable disease. Median duration of treatment is 20+ weeks and the longest is 58+ weeks.
Adverse events included rash (36%), fatigue (30%), nausea and vomiting (27%) and edema 20%).
There is an abstract on TSR-011 an inhibitor of ALK and TRK.
23 patients (10 NSCLC INCLUDING 5 ALK+). Doses have escalated from 30mg to 480mg. Maximum tolerated dose has been defined at a fractionated 60mg daily, which achives a sufficient trough concentration.
Of 5 patients with ALK+ NCSLC 3 (all Crizotinib resistant) achieved partial response.
Stable disease was observed in papillary thyroid, pancreatic, and colorectal patients.
There is an abstract for RXDX101 an inhibitor of TRK, ROS1, and ALK.
17 patients have been treated up to 1200mg/m2. Maximum tolerated dose has not been reached. Most common adverse events were paresthesias, nausea, dysgeusia, and diarrhea. No DLTs seen to date.
A patient with neuroblastoma (ALK+) had a partial response and is in cycle 13. Two patients had prolonged stabilization of disease and remain on treatment including a (ALK+ NSCLC PATIENT) in cycle 11.