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| Primary information |
|---|
| ID | 12524 |
| Therapeutic ID | Th1330 |
| Protein Name | Leronlimab |
| Sequence | >Th1330_Leronlimab
EVQLVESGGGLVKPGGSLRLSCAASGYTFSNYWIGWVRQAPGKGLEWIGDIYPGGNYIRNNEKFKDKTTLSADTSKNTAYLQMNSLKTEDTAVYYCGSSFGSNYVFAWFTYWGQGTLVTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLGK
|
| Molecular Weight | NA |
| Chemical Formula | NA |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | The half life of a 162mg subcutaneous dose is 3.4 days while the half life of a 324mg subcutaneous dose is 3.7 days.[A192846] |
| Description | Leronlimab, or PRO-140, is a human monoclonal antibody developed by CytoDyn.[L12684] It was first described in the literature in 2001.[A3922] This antibody binds to CCR5, which may be useful in treating HIV, cancers, and severely ill COVID-19 patients.[A192846,A192858,L12684] |
| Indication/Disease | Leronlimab is currently being investigated for the treatment of a number of cancers[A192858] and HIV.[A3922] Recently leronlimab has begun a phase II clinical trial in severely ill COVID-19 patients.[L12684] Preliminary data shows a reduction in the 'cytokine storm', particularly IL-6, as well as a normalization of the CD4/CD8 T-cell ratio.[L12684] These results may mitigate immune mediate injury seen in severely ill COVID-19 patients.[L12684] |
| Pharmacodynamics | Leronlimab is a humanized monoclonal antibody that binds CCR5 being investigated for it's anti-HIV, immunomodulatory, and anti-cancer effects.[A3922,A192858,L12684] |
| Mechanism of Action | CCR5 is a helical protein with multiple extracellular regions with adjacent G proteins.[A3922,A192858] When a chemokine binds CCR5, the Gaß trimer phosphorylates GDP to GTP and Ga dissociates.[A192858] Activated Ga activates adenylate cyclase, and increasing levels of cyclic AMP activate cytosolic protein kinase A.[A192858] Further downstream effects of CCR5 signalling include activation of NF-B and IL-6, as well as effects on cell proliferation, migration, and survival.[A192858,L12684] HIV enters cells expressing CD4 and a fusion coreceptor such as CCR5 and CXCR4.[A3922] Leronlimab is a monoclonal antibody which binds to multiple extracellular regions of the CCR5 receptor, preventing the entry of HIV into the cell.[A3922] Leronlimab's blocking of CCR5 is being investigated in cancer treatment, for it's effect on the cell cycle and immuno-modulation.[A192858] Leronlimab is also being investigated as a treatment for patients severely ill with COVID-19 due to it's effects on mitigating the cytokine storm and preventing immune-mediated injury.[L12684] |
| Toxicity | Data regarding overdose of leronlimab is not readily available. |
| Metabolism | Data regarding the metabolism of leronlimab is not readily available. However, as a monoclonal antibody it is expected to be degraded to smaller proteins and amino acids by proteolytic enzymes. |
| Absorption | A 162mg subcutaneous dose reaches a Cmax of 6.1mg/L, with a Tmax of 32 hours, and an AUC of 24.4mg |
| Data regarding the volume of distribution of leronlimab is not readily available. |
| Clearance | Data regarding the clearance of leronlimab is not readily available. |
| Categories | Experimental Unapproved Treatments for COVID-19 |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | C-C chemokine receptor type 5 |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |