Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function, for example conditions associated with pain. The compounds are 10,11-modified saxitoxins. The compounds are optionally additionally modified at carbon 13. In certain embodiments, the 10,11-modified saxitoxins are of Formula I: where R1, R2 and R3 are as described herein. Also provided herein are methods of treating pain in a mammal comprising administering an effective treatment amount of a 10,11 modified saxitoxin or composition to a mammal. In an embodiment, the mammal is a human.
