Drug name
Last update: Aug 2026Ibalizumab
Developer(s)
Drug information
Ibalizumab
Trogarzo
Biotherapeutic
mAb targeting gp120-CD4 complex
Ibalizumab (ibalizumab-uiyk; TMB-355; TNX-355) is a first-in-class humanised IgG4 monoclonal antibody indicated for use in heavily treatment experienced individuals with multidrug-resistant HIV-1 infection. Ibalizumab functions as a post-attachment inhibitor, specifically disrupting HIV-1 viral entry into CD4 cells through targeting of the gp120-CD4 complex. It binds to an epitope within domain 2 of the CD4 receptor, preventing the conformational changes necessary for co-receptor binding and subsequent fusion. Notably, Ibalizumab's binding site is distinct from both the gp120 and MHC-II binding regions, ensuring that it does not disrupt MHC-II mediated immune function. Additionally, Ibalizumab also acts to directly inhibit HIV-1 induced syncytium formation, further limiting viral spread.
Ibalizumab-uiyk (TROGARZO) 300mg/2mL (delivers 1.33ml) intravenous injection was approved for the treatment of heavily treated, multi-drug resistant HIV-1 infection in combination with other antiretroviral therapies. TROGARZO is currently approved only in the United States of America. Ibalizumab-uiyk (TROGARZO) was initially approved in the European Union, but later it was withdrawn from the EU market by the Marketing Authorization Holder for commercial reasons.
Ibalizumab-uiyk (TROGARZO) 300 mg/2 mL vial has received the Orphan Drug designation from the US FDA.
Therapeutic area(s)
- HIV
- Treatment
Administration route
Subcutaneous, Intramuscular, Intravenous
Associated long-acting platforms
Recombinant humanized monoclonal antibody
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
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Associated compounds, formulations and regimens
Not provided
Associated technologies
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Additional information
Developer(s)
Theratechnologies
Ibalizumab was initially developed by Biogen. In the late 1990s, Tanox acquired the exclusive global rights. Subsequently, Genentech acquired Tanox inheriting the ibalizumab license and later partnering with TaiMed Biologics. In 2012, TaiMed contracted WuXi PharmaTech to manufacture ibalizumab. Finally, in 2016, TaiMed established a collaboration with Theratechnologies for commercialization.
TaiMed Biologics
TaiMed Biologics is a highly specialized biopharmaceutical company headquartered in Taiwan that focuses on the development and commercialization of HIV therapeutics. TaiMed was originally founded in Sep 2007 after securing an exclusive license agreement with Genentech for the anti-cd4 antibody Ibalizumab (TMB-355). In March 2018, TMB-355 was approved by the U.S FDA under the brand name Trogarzo®.
Drug structure
Scale-up and manufacturing prospects
Ibalizumab is a humanised IgG4, κ monoclonal antibody produced in a NS0 cell line. The successful scale-up of therapeutic monoclonal antibody (mAb) products involves achieving favourable pharmacokinetic profiles, maintaining formulation stability and ensuring consistency of the overall product quality. However, industrial bioprocessing steps can potentially introduce additional complexities regarding mAb solution viscosity and aggregation propensity.
Industrial bioreactor vessel with a production volume capacity of between 5-25kL. Continuous disc stack centrifuges for bioreactor harvesting with subsequent membrane and depth filtration for supernatant clarification. Recombinant protein-A chromatography or other suitable affinity capture apparatus followed by two chromatographic polishing steps such as cation- and anion-exchange. Ultrafiltration membrane system to concentrate and formulate the final product.
Store in a refrigerator at 2ËšC to 8ËšC (36ËšF to 46ËšF). Protect from light until use. Do not freeze. Ibalizumab is supplied in a single 2 mL (200mg/1.33 mL) glass vial with a rubber stopper and aluminum flip-off seal. MAbs are highly dependent on their structural, chemical and conformational stability for biological activity. Chemical degradation of mAbs during manufacture can lead to the generation of product variants and complex impurity profiles. Additionally prior to packaging, the final product requires close monitoring for the presence of residual contaminants such as endotoxins.
Formulation characterisation steps for therapeutic mAb products include (but are not limited to): (1) Identification of post-translational modifications using ion-exchange chromatography and capillary isoelectric focusing. (2) Measurement of concentration dependent aggregation rates via thermal differential scanning calorimetry, sub-visible particle quantitation and size-exclusion chromatography. (3) Antibody clipping and fragmentation detection by capillary electrophoresis.
Excipients & delivery device(s)
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No delivery device
Safety, Efficacy and Evidence Summary
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Use of ibalizumab for the treatment of HIV-2 infection
There are major differences in the susceptibility of human immunodeficiency virus type 1 (HIV-1) and human immunodeficiency virus type 2 (HIV-2) to currently available drugs, and novel approaches for the treatment of HIV-2 are needed. The present application relates to a method for treating infection by several HIV-2 strains/isolates, including multidrug resistant (MDR) HIV-2 strains, comprising administering to a subject in need thereof an effective amount of ibalizumab, or of an antibody or antigen-binding fragment thereof that binds the same antigenic epitope, or an overlapping epitope, as ibalizumab.
WO2021062546
Use
Taimed biologics inc.
Not provided
October 1, 2040
Not entered into national phase
Ibalizumab and homologues (anti-CD4 antibodies blocking HIV-induced syncytia)
Anti-CD4 antibody homologs, DNA sequences and recombinant DNA molecules encoding them, prophylactic, immunotherapeutic and diagnostic compositions comprising those antibody homologs, and methods for preventing or treating diseases in mammals, including humans, caused by infective agents whose primary targets are CD4+ lymphocytes. Such diseases include acquired immune deficiency syndrome ('AIDS'), AIDS related complex, and human immunodeficiency virus infection.
WO1992009305
Compound patent broad claims and CDR
Biogen
Not provided
November 27, 2011
Expired