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

General Information of Drug (ID: DM6H10N)

• Drug Name: PUR1800 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Chronic obstructive pulmonary disease	CA22	Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DM6H10N

Molecule-Related Drug Atlas

Drug(s) Targeting Stress-activated protein kinase (p38)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-07265803	DM3E6Q4	Dilated cardiomyopathy	BC43.0	Phase 3	[3]
ARRY-797	DMJ48AB	Dilated cardiomyopathy	BC43.0	Phase 2	[4]
BMS-582949	DMGYXFP	Atherosclerosis	BD40	Phase 2	[5]
AZD7624	DMEW3K9	Chronic obstructive pulmonary disease	CA22	Phase 2	[6]
GSK2269557	DMIN0SV	Asthma	CA23	Phase 2	[7]
TAK-715	DMZKPI8	Rheumatoid arthritis	FA20	Phase 2	[8]
MW150	DMBRVXB	Alzheimer disease	8A20	Phase 2	[9]
LY-2228820	DMHXTNW	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[10]
ARRY-614	DMXD93K	Arthritis	FA20	Discontinued in Phase 1	[11]
TA-5493	DMFES2K	Inflammation	1A00-CA43.1	Discontinued in Phase 1	[12]

Drug(s) Targeting Tyrosine-protein kinase SYK (SYK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fostamatinib	DM6AUHV	Immune thrombocytopenic purpura	3B64.13	Approved	[13]
Fostamatinib disodium	DM3274D	Thrombocytopenia	3B64	Phase 3	[4]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[14]
TAK-659	DMJH3U0	Diffuse large B-cell lymphoma	2A81	Phase 2	[15]
GS-9876	DM9Q2B6	Cutaneous lupus erythematosus	EB5Z	Phase 2	[16]
GS-9973	DMKWCTR	Acute myeloid leukaemia	2A60	Phase 2	[17]
Cevidoplenib	DM9QU5G	Rheumatoid arthritis	FA20	Phase 2	[18]
HM43239	DMV1SDA	Acute myeloid leukaemia	2A60	Phase 1/2	[19]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[20]
SKI-O-703	DMTSKXR	Rheumatoid arthritis	FA20	Phase 1	[16]

Drug(s) Targeting Proto-oncogene c-Src (SRC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[21]
Bosutinib	DMTI8YE	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[21]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[22]
Herbimycin A	DM6YWBF	Solid tumour/cancer	2A00-2F9Z	Approved	[23]
AL3818	DM3WP0N	Alveolar soft part sarcoma	2A60-2C35	Phase 3	[24]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[24]
Masitinib	DMRSNEU	Amyotrophic lateral sclerosis	8B60.0	Phase 3	[16]
KX-01	DMF0NA9	Actinic keratosis	EK90.0	Phase 3	[25]
Saracatinib	DMBLHGP	Hematologic tumour	2B33.Y	Phase 2	[26]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[27]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[2]
Stress-activated protein kinase (p38)	TTWELHI	NOUNIPROTAC	Inhibitor	[2]
Tyrosine-protein kinase SYK (SYK)	TTOU65C	KSYK_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT04759807) A Phase 1b 3-way Crossover Study to Assess the Safety, Tolerability and Pharmacokinetics of Repeated Once Daily Doses of PUR1800 in Adult Patients With Stable Chronic Obstructive Pulmonary Disease. U.S.National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Pulmatrix Lexington, MA
• [3] Clinical pipeline report, company report or official report of Pfizer
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38alpha inhibitor. Bioorg Med Chem Lett. 2013 May 15;23(10):3028-33.
• [6] Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.
• [7] Evaluation of WO2012032067 and WO2012055846: two selective PI3Kdelta inhibitors, which is GSK-2269557. Expert Opin Ther Pat. 2012 Aug;22(8):965-70.
• [8] Inhibition of Wnt/beta-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Idelta/ . Chem Biol. 2011 Apr 22;18(4):485-94.
• [9] p38alpha MAPK signaling drives pharmacologically reversible brain and gastrointestinal phenotypes in the SERT Ala56 mouse. Proc Natl Acad Sci U S A. 2018 Oct 23;115(43):E10245-E10254.
• [10] 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. (Ligand id: 7959).
• [11] Cmpany report (Arraybiopharma)
• [12] US patent application no. 2008,0269,123, Methods for treating polycystic kidney disease (pkd) or other cyst forming diseases.
• [13] 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: 2230).
• [14] Company report (Portola Pharmaceuticals)
• [15] J Clin Oncol 32:5s, 2014 (suppl; abstr 8580).
• [16] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [17] An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Apr 9;125(15):2336-43.
• [18] A novel selective spleen tyrosine kinase inhibitor SKI-O-703 (cevidoplenib) ameliorates lupus nephritis and serum-induced arthritis in murine models. Clin Exp Immunol. 2023 Mar 8;211(1):31-45.
• [19] Clinical pipeline report, company report or official report of Hanmi Pharmaceutical.
• [20] The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324.
• [21] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [22] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [23] In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
• [24] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [25] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [26] Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
• [27] Clinical pipeline report, company report or official report of Turning Point Therapeutics.