Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTBID49)

• DTT Name: C-X-C chemokine receptor type 4 (CXCR4) DTT Info
• Gene Name: CXCR4

Molecule-Related Drug & Molecule List

2 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Motixafortide	DMW34B1	Multiple myeloma	2A83	Approved	[1]
Plerixafor	DMCJN1P	Non-hodgkin lymphoma	2B33.5	Approved	[2]

14 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMD-070	DMVOY6B	Whim syndrome	4A00.Y	Phase 3	[3]
Balixafortide	DMUOFAC	Metastatic breast cancer	2C6Y	Phase 3	[4]
Ulocuplumab	DM6PMNR	Multiple myeloma	2A83	Phase 3	[5]
POL-6326	DM4OT29	Human immunodeficiency virus infection	1C62	Phase 2	[6]
TG-0054	DM2ZLWH	Macular degeneration	9B78.3	Phase 2	[7]
CTCE-9908	DM95XR8	Sarcoma	2A60-2C35	Phase 1/2	[8]
USL311	DM6HPEC	Recurring respiratory infection	CA07-CA45	Phase 1/2	[9]
ALX-0651	DMIRYM8	Haematological malignancy	2B33.Y	Phase 1	[10]
BMS-936564	DMS4H1J	Acute myeloid leukaemia	2A60	Phase 1	[11]
CTCE-0214	DM2HES0	Constitutional neutropenia	4B00.0	Phase 1	[12]
GMI-1359	DML1KSA	Breast cancer	2C60-2C65	Phase 1	[13]
LY2624587	DM289Z4	Metastatic cancer	2D50-2E2Z	Phase 1	[14]
MSX-122	DM1N9YS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
PF-06747143	DM2ZJ1C	Acute myeloid leukaemia	2A60	Phase 1	[5]

3 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Garnocestim	DMCZAJW	Bone marrow transplantation	QB63.6	Discontinued in Phase 1	[16]
SURADISTA	DM1Z42H	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[17]
KRH-2731	DM2L0VF	Human immunodeficiency virus infection	1C62	Terminated	[19]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MAb173	DM5IMAU	Kaposi sarcoma	2B57	Preclinical	[18]

41 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AT-009	DMCO2S4	Solid tumour/cancer	2A00-2F9Z	Investigative	[20]
ATI-2341	DMLDWHP	Bone marrow transplantation	QB63.6	Investigative	[20]
CTCE-0324	DMEGZHF	Peripheral vascular disease	BD4Z	Investigative	[20]
CX-02	DMXMIT4	Solid tumour/cancer	2A00-2F9Z	Investigative	[20]
CXCL8	DMG1SXD	Psoriasis vulgaris	EA90	Investigative	[21]
CXCR4 gene disrupted T cells	DMNSUD9	Human immunodeficiency virus infection	1C62	Investigative	[20]
Cyclo(-D-Ala-D-Arg-L-Arg-L-Nal-Gly-)	DMLY8CU	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-MeTyr-D-Arg-L-Arg-L-Nal-Gly-)	DMBKRQ9	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-MeTyr-L-Arg-L-Arg-L-Nal-Gly-)	DMHI0UL	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-Arg-Arg-Nal-Gly-)	DM82C6Q	Discovery agent	N.A.	Investigative	[23]
Cyclo(-D-Tyr-D-Ala-L-Arg-L-Nal-Gly-)	DM8RKT1	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-MeNal-Gly-)	DM8XVAW	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-beta-Ala-)	DMWFITM	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-D-Ala-)	DMSA0IW	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-Gly-)	DMGOW1E	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-L-Ala-)	DM3PRHF	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-L-Pic-)	DMS9QHI	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-Sar-)	DM3Y1TZ	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-Arg-L-MeArg-L-Nal-Gly-)	DMUWC5O	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-D-MeArg-L-Arg-L-Nal-Gly-)	DM8F5DY	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Ala-L-Arg-L-Nal-Gly-)	DMPW9SD	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-Ala-Sar-)	DMOWT4H	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-MeNal-Gly-)	DMPZ316	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-beta-Ala-)	DMNQWBS	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-D-Ala-)	DMV6C9N	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-Gly-)	DMH9VMO	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-L-Ala-)	DM72HW3	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-Arg-L-MeArg-L-Nal-Gly-)	DMSPKWD	Discovery agent	N.A.	Investigative	[22]
Cyclo(-D-Tyr-L-MeArg-L-Arg-L-Nal-Gly-)	DMIUVQ6	Discovery agent	N.A.	Investigative	[22]
GSK-812397	DMT98PA	Human immunodeficiency virus-1 infection	1C62	Investigative	[20]
isothiourea-1a	DMAYOTF	Discovery agent	N.A.	Investigative	[24]
isothiourea-1t	DMBX4WR	Discovery agent	N.A.	Investigative	[24]
KUR-CXCR4	DMPKDJ4	Discovery agent	N.A.	Investigative	[20]
LP-0067	DMWTJ3E	Autoimmune diabetes	5A10	Investigative	[20]
NB-325	DM7K36E	Human immunodeficiency virus infection	1C62	Investigative	[20]
ND-401	DMT0NQS	Human immunodeficiency virus infection	1C62	Investigative	[20]
T134	DM6HZVC	Discovery agent	N.A.	Investigative	[25]
T140	DMIHBC5	Discovery agent	N.A.	Investigative	[25]
T22	DMBIH8A	Discovery agent	N.A.	Investigative	[25]
TN-14003	DME0I7O	Acute lymphoblastic leukaemia	2A85	Investigative	[26]
viral macrophage inflammatory protein-II	DMAXOPS	Discovery agent	N.A.	Investigative	[27]

References

• [1] The CXCR4 Antagonist BL-8040 Efficiently Induces Apoptosis and Inhibits The Survival Of AML Cells. November 15, 2013; Blood: 122 (21).
• [2] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [3] Pharmacokinetic effect of AMD070, an Oral CXCR4 antagonist, on CYP3A4 and CYP2D6 substrates midazolam and dextromethorphan in healthy volunteers. J Acquir Immune Defic Syndr. 2008 Apr 15;47(5):559-65.
• [4] Anti-ageing pipeline starts to mature.Nat Rev Drug Discov. 2018 Sep;17(9):609-612.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] CXCR4 inhibitors: tumor vasculature and therapeutic challenges. Recent Pat Anticancer Drug Discov. 2012 Sep;7(3):251-64.
• [7] CXCR4 Antagonist TG-0054 Mobilizes Mesenchymal Stem Cells, Attenuates Inflammation, and Preserves Cardiac Systolic Function in a Porcine Model of Myocardial Infarction. Cell Transplant. 2015;24(7):1313-28.
• [8] A CXCR4 antagonist CTCE-9908 inhibits primary tumor growth and metastasis of breast cancer. J Surg Res. 2009 Aug;155(2):231-6.
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] Therapeutic antibodies directed at G protein-coupled receptors. MAbs. 2010 Nov-Dec; 2(6): 594-606.
• [11] BMS-936564/MDX-1338: a fully human anti-CXCR4 antibody induces apoptosis in vitro and shows antitumor activity in vivo in hematologic malignancies. Clin Cancer Res. 2013 Jan 15;19(2):357-66.
• [12] Beneficial effect of a CXCR4 agonist in murine models of systemic inflammation. Inflammation. 2012 Feb;35(1):130-7.
• [13] Clinical pipeline report, company report or official report of GlycoMimetics.
• [14] Inhibition of CXCR4 by LY2624587, a Fully Humanized Anti-CXCR4 Antibody Induces Apoptosis of Hematologic Malignancies. PLoS One. 2016 Mar 8;11(3):e0150585.
• [15] Comparative evaluation of CC chemokine-induced migration of murine CD8alpha+ and CD8alpha- dendritic cells and their in vivo trafficking. J Leukoc Biol. 2004 Feb;75(2):275-85.
• [16] CN patent application no. 101094684, With the combination of chemokine activation progenitor cells/stem cells.
• [17] Suradista NSC 651016 inhibits the angiogenic activity of CXCL12-stromal cell-derived factor 1alpha. Clin Cancer Res. 2002 Dec;8(12):3955-60.
• [18] Caspase-dependent apoptosis of cells expressing the chemokine receptor CXCR4 is induced by cell membrane-associated human immunodeficiency virus type 1 envelope glycoprotein (gp120). Virology. 2000 Mar 15;268(2):329-44.
• [19] Progress in targeting HIV-1 entry. Drug Discov Today. 2005 Aug 15;10(16):1085-94.
• [20] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 71).
• [21] Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci U S A. 2004 Aug 10;101(32):11791-6.
• [22] Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone... J Med Chem. 2007 Jan 25;50(2):192-8.
• [23] Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4124-9.
• [24] Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J Med Chem. 2008 Dec 25;51(24):7915-20.
• [25] A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140. Biochem Biophys Res Commun. 1998 Dec 30;253(3):877-82.
• [26] Discovery of small molecule CXCR4 antagonists. J Med Chem. 2007 Nov 15;50(23):5655-64.
• [27] A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science. 1997 Sep 12;277(5332):1656-9.