(Heavy chain)
QMQLVESGGG VVQPGRSLRL SCAASGFTFR TYGMHWVRQA PGKGLEWVAV IWYDGSNKHY
ADSVKGRFTI TRDNSKNTLN LQMNSLRAED TAVYYCARAP QWELVHEAFD IWGQGTMVTV
SSASTKGPSV FPLAPCSRST SESTAALGCL VKDYFPEPVT VSWNSGALTS GVHTFPAVLQ
SSGLYSLSSV VTVPSSNFGT QTYTCNVDHK PSNTKVDKTV ERKCCVECPP CPAPPVAGPS
VFLFPPKPKD TLMISRTPEV TCVVVDVSHE DPEVQFNWYV DGVEVHNAKT KPREEQFNST
FRVVSVLTVV HQDWLNGKEY KCKVSNKGLP APIEKTISKT KGQPREPQVY TLPPSREEMT
KNQVSLTCLV KGFYPSDIAV EWESNGQPEN NYKTTPPMLD SDGSFFLYSK LTVDKSRWQQ
GNVFSCSVMH EALHNHYTQK SLSLSPGK
(Light chain)
SYVLTQPPSV SVAPGQTARI TCGGNNLGSK SVHWYQQKPG QAPVLVVYDD SDRPSWIPER
FSGSNSGNTA TLTISRGEAG DEADYYCQVW DSSSDHVVFG GGTKLTVLGQ PKAAPSVTLF
PPSSEELQAN KATLVCLISD FYPGAVTVAW KADSSPVKAG VETTTPSKQS NNKYAASSYL
SLTPEQWKSH RSYSCQVTHE GSTVEKTVAP TECS
(Disulfide bridge: H22-H96, H136-L213, H149-H205, H224-H’224, H225-H’225, H228-H’228, H231-H’231, H262-H322, H368-H426, H’22-H’96, H’136-L’213, H’149-H’205, H’262-H’322, H’368-H’426, L22-L87, L136-L195, L’22-L’87, L’136-L’195)
Tezepelumab-ekko
テゼペルマブ (遺伝子組換え)
| Formula | C6400H9844N1732O1992S52 |
|---|---|
| CAS | 1572943-04-4 |
| Mol weight | 144588.4306 |
PEPTIDE
UD FDA APPROVED, 12/17/2021, To treat severe asthma as an add-on maintenance therapy , Tezspire
Monoclonal antibody
Treatment of asthma and atopic dermatitis
Tezepelumab, sold under the brand name Tezspire, is a human monoclonal antibody used for the treatment of asthma.[4][5]
It blocks thymic stromal lymphopoietin (TSLP),[2] an epithelial cytokine that has been suggested to be critical in the initiation and persistence of airway inflammation.[6]
It was approved for medical use in the United States in December 2021.[2][3]
Medical uses
Tezepelumab is indicated for the add-on maintenance treatment of people aged twelve years and older with severe asthma.[2]
Research
In Phase III trials, tezepelumab demonstrated efficacy compared to placebo for patients with severe, uncontrolled asthma.[7][8]
Structural studies by X-ray crystallography showed that Tezepelumab competes against a critical part of the TSLPR binding site on TSLP.[1]
It is being studied for the treatment of chronic obstructive pulmonary disease, chronic rhinosinusitis with nasal polyps, chronic spontaneous urticaria and eosinophilic esophagitis (EoE).[3]
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References
- ^ Jump up to:a b Verstraete K, Peelman F, Braun H, Lopez J, Van Rompaey D, Dansercoer A, et al. (April 2017). “Structure and antagonism of the receptor complex mediated by human TSLP in allergy and asthma”. Nature Communications. 8 (1): 14937. Bibcode:2017NatCo…814937V. doi:10.1038/ncomms14937. PMC 5382266. PMID 28368013.
- ^ Jump up to:a b c d https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/761224s000lbl.pdf
- ^ Jump up to:a b c “Tezspire (tezepelumab) approved in the US for severe asthma”. AstraZeneca (Press release). 17 December 2021. Retrieved 17 December 2021.
- ^ Marone G, Spadaro G, Braile M, Poto R, Criscuolo G, Pahima H, et al. (November 2019). “Tezepelumab: a novel biological therapy for the treatment of severe uncontrolled asthma”. Expert Opinion on Investigational Drugs. 28 (11): 931–940. doi:10.1080/13543784.2019.1672657. PMID 31549891. S2CID 202746054.
- ^ Matera MG, Rogliani P, Calzetta L, Cazzola M (February 2020). “TSLP Inhibitors for Asthma: Current Status and Future Prospects”. Drugs. 80 (5): 449–458. doi:10.1007/s40265-020-01273-4. PMID 32078149. S2CID 211194472.
- ^ “Tezepelumab granted Breakthrough Therapy Designation by US FDA”. AstraZeneca (Press release). 7 September 2018.
- ^ “Studies found for: Tezepelumab”. ClinicalTrials.Gov. National Library of Medicine, National Institutes of Health, U.S. Department of Health and Human Services.
- ^ Menzies-Gow A, Corren J, Bourdin A, Chupp G, Israel E, Wechsler ME, et al. (May 2021). “Tezepelumab in Adults and Adolescents with Severe, Uncontrolled Asthma”. New England Journal of Medicine. 384 (19): 1800–09. doi:10.1056/NEJMoa2034975. PMID 33979488. S2CID 234484931.
External links
- “Tezepelumab”. Drug Information Portal. U.S. National Library of Medicine.
- Clinical trial number NCT02054130 for “Study to Evaluate the Efficacy and Safety of MEDI9929 (AMG 157) in Adult Subjects With Inadequately Controlled, Severe Asthma” at ClinicalTrials.gov
- Clinical trial number NCT03347279 for “Study to Evaluate Tezepelumab in Adults & Adolescents With Severe Uncontrolled Asthma (NAVIGATOR)” at ClinicalTrials.gov
| Structural basis for inhibition of TSLP-signaling by Tezepelumab (PDB 5J13)[1] | |
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | thymic stromal lymphopoietin (TSLP) |
| Clinical data | |
| Trade names | Tezspire |
| Other names | MEDI9929, AMG 157, tezepelumab-ekko |
| License data | US DailyMed: Tezepelumab |
| Routes of administration | Subcutaneous |
| ATC code | None |
| Legal status | |
| Legal status | US: ℞-only [2][3] |
| Identifiers | |
| CAS Number | 1572943-04-4 |
| DrugBank | DB15090 |
| ChemSpider | None |
| UNII | RJ1IW3B4QX |
| KEGG | D11771 |
| Chemical and physical data | |
| Formula | C6400H9844N1732O1992S52 |
| Molar mass | 144590.40 g·mol−1 |
////////////Tezepelumab-ekko, Tezspire, PEPTIDE, APPROVALS 2021, FDA 2021, Monoclonal antibody
, asthma, atopic dermatitis, ANTI INFLAMATORY, テゼペルマブ (遺伝子組換え)
