The present disclosure relates generally to supramolecular combinatorial therapeutics, compositions comprising same, and uses thereof. In particular, the present disclosure provides hydrophobic taxane-lipid covalent conjugates which create supramolecular assembly, for example, within lipid bilayer, providing an extra stabilization resulting in increased intratumoral concentration and hence increased efficacy. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a taxane-lipid conjugate is combined with one or more of a platinum compound, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid.
