To be observed and analyzed by the network of current gravitational wave detectors (LIGO, Virgo, KAGRA), and in anticipation of future third generation ground based (Einstein Telescope, Cosmic Explorer) and space borne (LISA) detectors, inspiralling compact binaries -- binary star systems composed of neutron stars and/or black holes in their late stage of evolution prior the final coalescence -- require high-accuracy predictions from general relativity. The orbital dynamics and emitted gravitational waves of these very relativistic systems can be accurately modelled using state-of-the-art post-Newtonian theory. In this article we review the Multipolar-Post-Minkowskian approximation scheme, merged to the standard Post-Newtonian expansion into a single formalism valid for general isolated matter system. This cocktail of approximation methods (called MPM-PN) has been successfully applied to compact binary systems, producing equations of motion up to the fourth-post-Newtonian (4PN) level, and gravitational waveform and flux to 4.5PN order beyond the Einstein quadrupole formula. We describe the dimensional regularization at work in such high post-Newtonian calculations, for curing both ultra-violet and infra-red divergences. Several landmark results are detailed: the definition of multipole moments, the gravitational radiation reaction, the conservative dynamics of circular orbits, the first law of compact binary mechanics, and the non-linear effects in the gravitational wave propagation (tails, iterated tails and non-linear memory). We also discuss the case of compact binaries moving on eccentric orbits, and the effects of spins (both spin-orbit and spin-spin) on the equations of motion and gravitational wave energy flux and waveform.