psma

PSMA-11 (HBED-CC-PSMA) detects prostate cancer recurrence and metastasis by binding to the extracellular structural domain of prostate-specific membrane antigen (PSMA).PSMA-11 is often used as a tracer of PSMA-expressing tumours in positron emission tomography (PET) scanning by intravenous injection of gallium Ga 68-labelled PSMA-11, Glu-urea-Lys(Ahx) molecule targeted and bound PSMA-expressing tumour cells. After internalisation, PSMA-expressing tumour cells could be detected on PET imaging.

PSMA-ALB-56 is a PSMA-targeting radioactive ligand with antitumor activity, composed of glutamic urea PSMA binding entities, DOTA chelating agents, and albumin binders based on 4-(p-iodophenyl)- fragment or p(tolyl)- fragment.

PSMA–DA1 may be a useful PSMA-targeting radiotheranostic agent.

PSMA-1007 is a novel Glu-Ureido-type prostate-specific membrane antigen (PSMA) inhibitor.

Vipivotide tetraxetan (PSMA-617) is a highly potent inhibitor of prostate-specific membrane antigen (PSMA) with a Ki of 0.37 nM.

Zadavotide guraxetan (PSMAI&T; PNT-2002) is an inhibitor of prostate-specific membrane antigen (PSMA) with potential antitumor activity, and it is useful for research targeting prostate cancer.

PNT2001 (LY4181530) is an effective prostate-specific membrane antigen (PSMA) ligand with an IC50 of 3.1 nM. It enhances cellular internalization and, when labeled with 177Lu and 225Ac, is applicable for prostate cancer research.

PSMA-D5 exhibits a binding affinity for PSMA with a Ki of 0.21 nM and becomes useful for PSMA tracing following radiolabeling. When marked with [68Ga], PSMA-D5 contains a DOTA chelator, facilitating the convenient labeling with therapeutic radionuclides such as 177Lu and 225Ac. Additionally, [68Ga]-labeled PSMA-D5 demonstrates exceptional pharmacokinetic properties and significant tumor uptake in 22Rv1 tumors. This compound can be employed in the synthesis and research of radiolabeled conjugates (RDC).

PSMAbinder-3 is a ligand for PSMA.

PSMA-trillium is a PSMA-targeting compound comprising a PSMA-targeting molecule (PSMA binding agent), a Macropa chelator, and a pharmacokinetics-modulating group (PK modulator). It acts as the non-radioactive variant of Actinium-225-PSMA-Trillium (BAY 3563254), boasting enhanced PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind with Ac through either the Macropa chelator or the radioactive isotope Actinium-225. Actinium-225-PSMA-Trillium effectively inhibits metastatic castration-resistant prostate cancer (mCRPC).

PSMAligand 1 (Compound 1c) is a PSMA ligand with an IC50 of 26.74 nM. When labeled with [18F], PSMAligand 1 serves as a PSMAPET tracer for research related to the diagnosis of prostate cancer.

PSMA-DIM is a dimeric PSMA ligand with a Kd value of 37.09 nM for LNCaP cells. It can be radiolabeled with [68Ga]Ga to form [68Ga]Ga-PSMA-DIM, which effectively differentiates cells and animal models with varying PSMA expression levels. [68Ga]Ga-PSMA-DIM exhibits high uptake in LNCaP cells and maximizes tumor uptake. PSMA-DIM is applicable in prostate cancer (PCa) research.

PSMA617-TCMC is a derivative of PSMA-617 with structure modification, in which the caroboxy groups in DOTA ring is replaced by TCMC macrocycle. PSMA-617 is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.

PSMA I&T is a PSMA-targeting radiocompound that serves as a diagnostic agent for prostate-specific membrane antigen-targeted therapy, often coupled with radioactivity.

PSMA-IN-3 (compound 17) is a novel, high-affinity inhibitor of Prostate-Specific Membrane Antigen (PSMA) with an IC50 of 13 nM, showing potential for development as an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer [1].

PSMA-Val-Cit-PAB-Azide, a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), incorporates a cleavable linker (Val-Cit-PAB) and a novel small-molecule conjugate targeting PSMA. This compound features an Azide group, enabling it to participate in the copper-catalyzed azide-alkyne cycloaddition reaction (CuAAC) with Alkyne-group-containing molecules [1].

Anti-PSMA Antibody is a humanized IgG1 monoclonal antibody targeting PSMA. It serves as the antibody component of the ADC molecule ARX517.

EB-PSMA-617 is an advanced version of PSMA-617, designed to enhance pharmacokinetic properties through conjugation with Evans Blue (EB), thereby extending its circulation half-life for improved prostate tumor targeting and radiotherapy effectiveness. In preclinical studies with PC3-PIP-loaded mice, EB-PSMA-617 showed an extended blood half-life, greater accumulation in PSMA-positive tumors, and effective tumor elimination with reduced radioactivity.

PSMA/GRPR ligand 1 (compound 3) is a bispecific ligand with dual targeting capabilities for tumors that express PSMA(+) and GRPR(+).

PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. It inhibits tumor growth with high selectivity and specificity in PSMA+ tumor models. Additionally, PSMA-IN-1 serves as an NIR (λEX: 620 nm; λEM: 670 nm) dye for tumor imaging. PSMA-IN-1 is utilized in prostate cancer research.

DOTA-PSMA-EB-01 (Compound LNC1003) is a specific inhibitor of PSMA with an IC50 of 10.77 nM. It enhances tumor uptake and retention of 177Lu. DOTA-PSMA-EB-01 is applicable in the synthesis or research of radiolabeled conjugates (RDC).

Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.

Vipivotide tetraxetan Linker (PSMA-617 Linker) is a noncleavable peptide linker utilized in the synthesis of Vipivotide tetraxetan (PSMA-617), a ligand instrumental in producing 177Lu-PSMA-617. This radioactive molecule is applied in the treatment of prostate cancer[1].

REGN5678 is a bispecific antibody that targets both PSMA on prostate cancer cells and CD28 on T cells, enhancing immune activation. This drug is being developed to treat prostate cancer by redirecting T cells to tumors expressing PSMA, thereby promoting tumor cell death. Its molecular weight is 145.86 kDa.