He blasted off from Baikonur Cosmodrome in Kazakhstan early on Thursday morning, and should arrive at the ISS on Saturday morning.
It makes him the first African to enter into space and the second "space tourist" to pay for the pleasure.
Mr Shuttleworth is an internet millionaire and had to undergo extensive training for his trip.
He even learnt Russian to aid communication with mission controllers in Moscow.
And we're giving you the chance to chat live with him next week - come back soon for more info!