Folate receptor binding ligand-drug conjugate

The invention provides a folate receptor binding ligand-drug conjugate. The conjugate is composed of a vitamin receptor binding part (F)n, a linker (L), and a drug or its analog or derivative (D), wherein n is an integer in a range of 2-4. The vitamin receptor binding part preferably selects folic acid or technical pteroic acid, the linker (L) comprises a multivalent linker L1 and at least one releasable linker L2, the (F)n is covalently connected to the multivalent linker L1, the drug or its analog or derivative (D) is covalently connected with the releasable linker L2, and the L1 is covalently connected with the L2. The conjugate provided by the invention has great improved affinity to folate receptor positive tumor cells, has substantial antitumor activity and has obviously reduced side effects.