Table 2.

Ex20 ins inhibitors.

Ex20 Inhibitor	Trial	Toxicity	Response to Treatment
Poziotinib	NCT03066206	Diarrhea 92%, skin rash 90%, oral mucositis 68%, paronychia 68%, dry skin 60% (66% of G3 AEs on EAP)	ORR 32%, mPFS 5.5 m, mOS 19.2 m ORR of 46% and 0% in near (aa A767 to P772) vs. far loop ins
Mobocertinib	NCT02716116	PPP cohort 69% G ≥ 3 AEs 46% SAE EXCLAIM cohort 66% G ≥ 3 AEs 44% SAE	PPP cohort ORR 28% by IRC and 35% by investigator assessment, mPFS 7.3 m by IRC, mOS 24.0 m EXCLAIM cohort ORR 25% by IRC and 32% by investigator assessment
Amivantamab	NCT02609776	At RP2D 39% G ≥ 3 AEs, 31% SAE	ORR 40%, mPFS 8.3 m
Sunvozertinib (DZD9008)	NCT03974022 and CTR20192097	Most common TEAEs: diarrhea (G3 5.2%) and skin rash (G3 1%)	ORR 39.3% across all dose levels; dose level of 300 mg once daily, ORR 48.4% and DCR 90.3%
CLN-081 (TAS6417)	NCT04036682	Constipation 8%, diarrhea 8%, dizziness 8%, fatigue 8%, and chest pain 8%	5 evaluable pts: 2 pts PR, 3 pts SD
Tarloxotinib	NCT03805841	G3 TEAEs: prolonged QTc 34.8%, rash 4.3%, diarrhea 4.3%, increased ALT 4.3%	DCR 60%

AEs: adverse events; EAP: expanded access program; ORR: objective response rate; mPFS: median progression-free survival; mOS: median overall survival; aa: amino acids; PPP: platinum-pretreated patients; SAE: severe adverse event; IRC: independent review committee; RP2D: recommended phase II dose; PR: partial response; SD: stable disease; TEAEs: treatment-emergent adverse events; DCR: disease control rate.