The present invention relates to a pyrrolobenzodiazepine dimer prodrug and a ligand-linker conjugate compound thereof, a composition containing these, and therapeutic use thereof particularly as an anticancer drug. The stability of the compounds themselves and the stability thereof in plasma are excellent and the compounds are advantageous in terms of manifestation of toxicity, and thus the compounds are industrially useful in that it is possible to target proliferative diseases such as cancer, to perform a specific treatment, to maximize the drug efficacy, and to minimize the occurrence of side effects.

The disclosure relates to carrier particle-drug conjugates, including nanoparticle drug conjugates (NDC), that can be used in the delivery of a drug to a biological target (e.g., for targeted delivery of a cytotoxic drug to a cancer cell or tumor). Also disclosed are self-immolative linkers and linker-payload conjugates suitable for use in a carrier particle drug conjugate, and methods of making the same, and methods for treating cancer.

The present invention provides a solid dispersion of a rifamycin-nitroimidazole coupling molecule, comprising a rifamycin-nitroimidazole coupling molecule of a structure shown in formula I, a polymer carrier, functional excipient and a solvent. The polymer carrier is selected from one or a combination of more of PVP K30, PVP-VA64, HPC-L, HPMC E3, Soluplus and polymethacrylate. The functional excipient comprise one or a combination of more of sodium lauryl sulfate, meglumine, VE-TPGS and Tween 80. The solid dispersion of the rifamycin-nitroimidazole coupling molecule of the present invention can be used as a formulation of a drug for treating microbial infection.

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Provided herein are methods and compositions using a target moiety linked to an active agent, in particular an antimicrobial agent. Such methods and compositions are useful in treating, e.g., microbial infections, such as antibiotic-resistant bacterial infections. Provided herein are methods and compositions using a target moiety linked to an active agent, in particular an antimicrobial agent. Such methods and compositions are useful in treating, e.g., microbial infections, such as antibiotic-resistant bacterial infections.

The disclosure relates to nanoparticle drug conjugates (NDC) that comprise ultrasmall nanoparticles, folate receptor (FR) targeting ligands, and linker-drug conjugates, and methods of making and using them to treat cancer.

The disclosure relates to nanoparticle drug conjugates (NDC) that comprise ultrasmall nanoparticles, folate receptor (FR) targeting ligands, and linker-drug conjugates, and methods of making and using them to treat cancer.

The disclosure relates to nanoparticle drug conjugates (NDC) that comprise ultrasmall nanoparticles, folate receptor (FR) targeting ligands, and linker-drug conjugates, and methods of making and using them to treat cancer.

This disclosure relates to methods of functionalizing a nanoparticle, e.g., for conjugation to a targeting ligand and/or payload moiety, such as for the production of a nanoparticle drug conjugate (NDC).

Disclosed herein are compounds having the following Formula (I) or a pharmaceutically acceptable salt form thereof: B-L-C (I) wherein B is a bone-binding moiety; L is a linker; and C is a cationic steroid antimicrobial (CSA) moiety, pharmaceutical compositions comprising the compounds, and methods of using the compounds or pharmaceutical compositions for the treatment of an infection or osteomyelitis in a bone of a subject, promotion of bone formation in a subject, or treatment of bone cancer or metastatic bone cancer in a subject.

Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target (in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.