Pharmaceutical Development and Drug Discovery Research

Cross-Linkers

Crosslinkers are mainly used to connect antibodies and toxins. The linker that connects cytotoxic drugs to monoclonal antibodies is the core part of ADC. One of the biggest challenges in developing effective ADCs is to choose a suitable crosslinker. The crosslinker must be able to release the cytotoxic drug in an active form in or near the target cell. The crosslinker is the basis for the effective delivery of cytotoxic drugs by ADC and is also a key factor in determining the toxicity of ADC products. Premature release of drugs in the circulation can lead to systemic toxicity and a lower therapeutic index. The choice of linker usually depends on the target, the drug, the internalization and degradation of the antibody-antigen complex, and the properties of the drug used.

Enzyme Cleavable Linkers (Cleave Motif)

There are specific enzymes in the intracellular lysosomes and tumor microenvironment that can selectively cleave linkers. For example, cathepsins in lysosomes can hydrolyze peptide bonds, such as dipeptide or tetrapeptide linkers. Glycosidases that hydrolyze β-glucuronide and β-galactosidase, phosphatases that hydrolyze pyrophosphate and pyrophosphate, and sulfatases that hydrolyze sulfates.

Payload (Drug) Candidates

After ADC drugs enter the blood circulation, they bind to the target antigen receptors on the surface of tumor cells. The newly formed ADC-antigen complex is internalized and degraded by lysosomes, releasing the payload and inducing tumor cell death. The payload is an important component of ADCs, and its activity and physicochemical properties directly affect the anti-tumor efficacy of ADCs drugs. The ideal payload should have sufficiently high cytotoxicity, low immunogenicity, high stability, modifiable functional groups, bystander killing effect, appropriate water solubility, and the target should be intracellular. Common payloads include tubulin inhibitors and DNA damaging agents.

Prodrug Ingredients

Prodrug, also known as prodrug, refers to a class of compounds that are inactive or weakly active, which are converted into metabolites or parent drugs with pharmacological activity or significantly enhanced pharmacological activity through enzyme catalysis or non-enzymatic action in the body. Prodrugs can be divided into two categories: Carrier-linked prodrug: The parent drug is linked to the carrier by a covalent bond, and the drug is exerted after the carrier is removed by biodegradation or chemical reaction in the body. The carrier is usually lipophilic and can be a small molecule compound such as a fatty chain, polyethylene glycol, etc., or a large molecule compound such as albumin and antibodies. Bioprecursor prodrug: The active ingredient is chemically modified, and after a series of enzymatic conversions in the body, the parent drug is released to exert its efficacy.

Natural Polymers (for DDS)

Natural polymers refer to high molecular weight compounds extracted from nature, such as polysaccharides, proteins and nucleic acids from plants, animals or microorganisms. Due to their good biocompatibility, biodegradability and diverse functional properties, natural polymers are widely used in the preparation of drug carriers and the development of more efficient and safe drug delivery solutions.

Monomers for Synthetic Polymers (for DDS)

Monomers are small molecules that can be combined together to form polymers through chemical reactions such as polymerization. In DDS, these monomers are usually designed to have specific functions in order to play a specific role in the drug delivery process.

Polyethyleneglycols (PEG) (for DDS)

Polyethylene glycol is a synthetic polymer material widely used in drug delivery systems (DDS). Due to its unique physicochemical properties and good biocompatibility, PEG plays an important role in improving the solubility, stability and bioavailability of drugs.

PEGylation Reagents (for DDS)

PEGylation agents are used to improve the pharmacokinetic properties of drugs or other biomolecules by attaching PEG to them. PEG is a non-toxic, non-immunogenic polymer with high hydrophilicity and flexibility that can increase the solubility of molecules and reduce renal clearance, thereby prolonging the circulation time of drugs in the body. PEGylation agents provide an effective way to improve the pharmacokinetic properties, stability and biocompatibility of drugs in drug delivery systems.

Cyclodextrins (for DDS)

The application of cyclodextrin (CD) in drug delivery systems (DDS) is mainly reflected in its unique structure and function. Cyclodextrin is a type of cyclic oligosaccharide composed of D-pyranose glucose units connected by α-1,4-glycosidic bonds. It usually contains 6, 7, and 8 glucose units, which are called α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin, respectively. Due to its special cylindrical structure, the inner side of the cavity of cyclodextrin is hydrophobic and the outer side is hydrophilic. This structure enables cyclodextrin to encapsulate a variety of organic and inorganic small molecules to form inclusion complexes, thereby changing the properties of these molecules, which can effectively improve the solubility, bioavailability, and targeting of drugs.

Drug Delivery Systems (DDS) Research Reagents (Others)

Phospholipids (for DDS)

Lipids (Other) (for DDS)

Synthetic Polymers (for DDS)

Synthetic polymers have become key materials in the field of modern medicine due to their adjustable physicochemical properties, good biocompatibility and adaptability, and play an important role in drug delivery systems.

Chelating Agents (for DDS)

Chelators play an important role in drug delivery systems. These compounds are able to form stable complexes with metal ions, thereby modulating their bioavailability, improving drug stability, reducing toxicity, or enhancing the therapeutic effect of drugs.

Antimicrobial Ingredients

Antimicrobial ingredients are compounds that can inhibit or kill microorganisms (such as bacteria, fungi, viruses and protozoa).

Antiparasitic Ingredients, Antiprotozoal Ingredients, Antihelminthic Ingredients

Used in the study of therapeutic antiparasitic, antiprotozoal, and anthelmintic compounds.

Antiviral Research Reagents

Compounds used in the study of therapeutic antiviral drugs.

Antitumor Research Reagents

Compounds used to study therapeutic anti-tumor drugs.

Antihypertensive Ingredients

Compounds used in the study of therapeutic antihypertensive drugs.

Antilipemic Ingredients

Compounds used in the study of therapeutic lipid-lowering drugs.

Antithrombotic Ingredients

Compounds used in the study of therapeutic antithrombotic drugs.

Antidiabetic Ingredients

Compounds used in the study of therapeutic anti-diabetic drugs.

Neurotransmitter Agent Ingredients

Compounds used in the study of therapeutic neurotransmitter drugs.

Anti-inflammatory Ingredients

Compounds used in the study of therapeutic anti-inflammatory drugs.

Anti-allergic Ingredients

Compounds used in the study of therapeutic anti-allergy drugs.

Immunosuppressant Ingredients

Compounds used to study therapeutic immunosuppressants.

Anti-rheumatoid Arthritis Ingredients

Compounds used in the study of therapeutic agents against rheumatoid arthritis.

Anti-osteoporosis Ingredients

Compounds used in the study of therapeutic anti-osteoporosis drugs.

Pharmaceutical Research Reagents (Others)

Cosmetic Research Reagents

Compounds used to study cosmetics.

Antifungal Ingredients

Compounds used in the study of therapeutic antifungal drugs.

Contrast Medium Ingredients

Compounds used in the study of contrast agents.

Anti-Constipation Ingredients

Compounds used in the study of therapeutic anti-constipation drugs.