Table 3.
Ongoing clinical trials with selective FGFR inhibitors
| Agent | Phase | Clinicaltrials.gov | Description | Response rate | Disease stabilisation |
|---|---|---|---|---|---|
| AZD4547 | Phase I trial | NCT00979134 | FGFR1- and/or FGFR2-gene-amplified solid cancer (C1 cohort) [13] | 1/20 (5 %) | 9/20 (45 %) |
| FGFR1-amplified squamous NSCLC (C2 cohort) [15] | 1/15 (6.6 %) | 5/15 (33.3 %) | |||
| FGFR2-amplified gastric cancer (C3 cohort) [14] | 1/13 (7.6 %) | 4/13 (30.7 %) | |||
| AZD4547 | Phase I/II trial | NCT01824901 | FGFR1-amplified squamous NSCLC, randomised to docetaxel with or without AZD4547 | NA | NA |
| AZD4547 | Phase II trial | NCT01457846 | Gastric or lower-oesophageal cancer, FGFR2 polysomy or amplification, randomised to AZD4547 or paclitaxel [30] | NA | NA |
| AZD4547 | Phase I/II trial | NCT01202591 | Oestrogen receptor positive and FGFR1-amplified BC, randomised to AZD4547 plus fulvestrant or fulvestrant alone | NA | NA |
| AZD4547 | Phase I/II trial | NCT01791985 | Oestrogen receptor positive BC, FGFR1-amplified or not, randomised to AZD4547 plus anastrozole or letrozole versus exemestane alone | NA | NA |
| AZD4547 | Phase II study | NCT01795768 | FGFR1- or FGFR2-amplified HER2-negative BC, NSCLC and gastroesophageal cancer [31] | 3/9 (33 % in GC) 1/8 (12.5 % in BC) |
NA |
| AZD4547 | Phase II/III trial | NCT02154490 | Squamous NSCLC, randomised to GDC-0032, rilotumumab, erlotinib, MEDI4736, palbociclib, AZD4547 or docetaxel depending on screening genomic analysis | NA | NA |
| AZD4547 | Phase II trial | NCT02117167 | Squamous NSCLC, randomised to AZD2014, AZD4547, AZD5363, AZD8931, selumetinib or vandetanib depending on screening genomic analysis | NA | NA |
| BGJ398 | Phase I trial | NCT01004224 | FGFR1- or FGFR2-amplified or FGFR3-mutated advanced solid tumours [19] | NA | NA |
| FGFR1-amplified squamous NSCLC cohort [19] | 4/26 (15.4 %) | 9/26 (34.6 %) | |||
| BGJ398 | Phase II trial | NCT01820364 | Advanced melanoma, LGX818 followed by a rational combination with LGX818, MEK162, LEE011, BGJ398, BKM120 or INC280 | NA | NA |
| BGJ398 | Phase II trial | NCT02150967 | Advanced cholangiocarcinoma, with FGFR2 gene fusions or other FGFR alterations | NA | NA |
| BGJ398 | Phase II trial | NCT01975701 | FGFR-amplified, translocated or mutated recurrent glioblastoma | NA | NA |
| BGJ398 | Phase II trial | NCT02160041 | FGFR aberrant solid tumours and/or hematologic malignancies | NA | NA |
| BGJ398 | Phase I trial | NCT01928459 | PIK3CA-mutated advanced solid tumours, without FGFR1–3 alterations, treated with BGJ398 with BYL719 | NA | NA |
| BGJ398 | Phase II trial | NCT02159066 | Advanced melanoma, LGX818 plus MEK162 followed by a rational combination on progression with LEE011, BGJ398, BKM120 or INC280 | NA | NA |
| LY2874455 | Phase I trial | NCT01212107 | Advanced cancer with FGFR aberrations during dose-expansion cohort | NA | NA |
| JNJ-42756493 | Phase I trial | NCT01703481 | Advanced cancer with FGFR1, 2 or 4 amplification (dose-expansion cohort) [16] | 2/8 (25 %) | 4/8 (50 %) |
FGFR fibroblast growth factor receptor, NSCLC non-small-cell lung cancer, BC breast cancer, GC gastroesophageal cancer, PIK3C phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha, NA not available