LTX-315

DRACPC ID  DRACPC0088

Active Ingredients   LTX-315

Description  A peptide derived from human lactoferrin, with potential lytic and immunostimulating activities. Upon transdermal injection directly into the tumor, ruxotemitide may bind to the tumor cell membranes and subsequently lyse tumor cells, thereby inducing tumor cell necrosis. In turn, presentation of the tumor antigens to the immune system may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells. This may trigger an immune response against tumor associated antigens on tumors distant from the primary tumor. Human lactoferrin, a 692 amino acid glycoprotein, belongs to the transferrin family of metal-binding proteins.

Synonyms  Oncopore; Ruxotemitide; LTX-315

Type  Small Molecule

Disease  Lymphoma, Melanoma, Carcinoma, Breast Cancer

Classification

  

Peptide and derivative

Structure Information


Molecular Formula  C78H106N18O9

Molecular Weight  1439.8

Active Sequence  KKWWKKWXK

Sequence Length  9

Modification  X=Dip, N-terminal NH2

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-2,6-diaminohexanamido]hexanamido]-3-(1H-indol-3-yl)propanamido]-3-(1H-indol-3-yl)propanamido]hexanamido]hexanamido]-3-(1H-indol-3-yl)propanamido]-3,3-diphenylpropanamido]hexanamide

InChI  InChI=1S/C78H106N18O9/c79-38-18-13-30-57(84)71(98)90-62(35-15-20-40-81)73(100)93-66(44-52-47-87-59-32-11-8-28-55(52)59)76(103)95-65(43-51-46-86-58-31-10-7-27-54(51)58)75(102)92-63(36-16-21-41-82)72(99)91-64(37-17-22-42-83)74(101)94-67(45-53-48-88-60-33-12-9-29-56(53)60)77(104)96-69(78(105)89-61(70(85)97)34-14-19-39-80)68(49-23-3-1-4-24-49)50-25-5-2-6-26-50/h1-12,23-29,31-33,46-48,57,61-69,86-88H,13-22,30,34-45,79-84H2,(H2,85,97)(H,89,105)(H,90,98)(H,91,99)(H,92,102)(H,93,100)(H,94,101)(H,95,103)(H,96,104)/t57-,61-,62-,63-,64-,65-,66-,67-,69-/m0/s1

InChI_Key GGAKLYWEFZCVIT-TVEKFXMRSA-N

SMILES  NCCCC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CCCCN)=O)CCCCN)=O)CC1=CNC2=C1C=CC=C2)=O)CC3=CNC4=CC=CC=C34)=O)C(N[C@@H](CCCCN)C(N[C@H](C(N[C@@H](C(C5=CC=CC=C5)C6=CC=CC=C6)C(N[C@H](C(N)=O)CCCCN)=O)=O)CC7=CNC8=C7C=CC=C8)=O)=O

External Codes


PubChem CID  46200994

DrugBank Accession Number  DB12748

NCI Thesaurus Code  C90547  

UNII  75FBL12IZ7   GSRS

CAS  1345407-05-7



Drug approval


Drug indication
    LTX-315 has been used in trials studying the treatment of Cancer, Lymphoma, Melanoma, Carcinoma, and Breast Cancer, among others.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT01058616 Phase 1 Dose-escalation Study of LTX-315 in Patients With a Transdermally Accessible Tumour Cancer With Transdermal Accessible Tumour Phase 1 Treatment
NCT01986426 A Phase I, Open-label, Multi-arm, Multi-centre, Multi-dose, Dose Escalation Study of LTX-315 as Monotherapy or in Combination With Either Ipilimumab or Pembrolizumab in Patients With Transdermally Accessible Tumours Cancer; Melanoma; Breast Cancer; Head and Neck Cancer; Lymphoma; Triple-Negative Breast Cancer Phase 1 Treatment
NCT01223209 A Phase I, Combination, Immunologic Study of LTX-315 as Adjunct to GV1001 in Patients Following Curative Surgery for Carcinoma Carcinoma Phase 1 Treatment
NCT04796194 A Phase II Study of Intratumoral Injection of LTX-315 in Combination With Pembrolizumab in Patients With Percutaneously Accessible Lesions With Advanced Melanoma Refractory to Pembrolizumab Advanced Melanoma Phase 2 Treatment
NCT03725605 An Open Label Phase II Single Centre Study Investigating the Safety and Efficacy of LTX-315 and Adoptive T-cell Therapy in Patients With Advanced/Metastatic Soft Tissue Sarcoma (ATLAS-IT-04) Soft Tissue Sarcoma Phase 2 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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