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

General Information of Drug (ID: DMHXTAQ)

• Drug Name: Pazufloxacin Drug Info
• Synonyms: 127045-41-4; T-3761; UNII-4CZ1R38NDI; 4CZ1R38NDI; NCGC00167534-01; DSSTox_CID_26697; DSSTox_RID_81831; DSSTox_GSID_46697; Pazufloxacin [INN]; SMR000466380; CCRIS 7312; CAS-127045-41-4; T 3761; 127046-18-8; PZFX; Pazufloxacin (JAN/INN); SCHEMBL34460; 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (S)-; MLS000759513; MLS001424116; CHEMBL240163; DTXSID5046697; CHEBI:94700; HY-B0724B; HMS2051B05; HMS2090H07; BCP12954; LSM-5745; RKL10069; ZINC3779726; Tox21_112531; BDBM50248017; MFCD00865012; AKOS015900451; Tox21_112531_1; AC-3506; CCG-100919; DB11774; GM-1171; KS-5008; NC00169; NCGC00167534-02; (-)-(3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid; 7H-Pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 2,3-dihydro-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-, (S)-; AB0012715; D01153; AB00639918-07; AB00639918-09; AB00639918_10; Pazufloxacin, VETRANAL(TM), analytical standard; SR-01000759348; J-005457; Q3898423; SR-01000759348-4; (S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; (S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid; 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid,10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-, (3S)-; 7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylicacid,10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-

Indication

Disease Entry	ICD 11	Status	REF
Conjunctivitis	9A60	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 65957
  ChEBI ID: CHEBI:94700
  CAS Number: CAS 127045-41-4
  TTD Drug ID: DMHXTAQ

Molecule-Related Drug Atlas

Drug(s) Targeting Bacterial DNA gyrase (Bact gyrase)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Grepafloxacin	DMGLX0T	Chronic bronchitis	CA20.1	Approved	[4]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[5]
Levofloxacin	DMS60RB	Acute maxillary sinusitis		Approved	[5]
Gatifloxacin	DMSL679	Acute gonococcal cervicitis		Approved	[5]
Norfloxacin	DMIZ6W2	Acute gonococcal cervicitis		Approved	[5]
Ozenoxacin	DM6KZMG	Impetigo	1B72	Approved	[6]
Sparfloxacin	DMB4HCT	Bacterial infection	1A00-1C4Z	Approved	[5]
Gemifloxacin	DMHT34O	Bacterial infection	1A00-1C4Z	Approved	[5]
Besifloxacin	DMPHXMI	Ocular inflammation	9C61.24	Approved	[7]
Finafloxacin	DMZEONG	Urinary tract infection	GC08	Approved	[8]

Drug(s) Targeting Bacterial DNA topoisomerase 4A (Bact parC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Prulifloxacin	DMOK965	Urinary tract infection	GC08	Approved	[9]
Sitafloxacin	DMTV5XC	Escherichia coli infection	1A03	Phase 2/3	[10]
VB 1953	DM0YWQ4	Acne vulgaris	ED80	Phase 2	[11]
JNJ-32729463	DMQD1GN	Community-acquired pneumonia	CA40.Z	Phase 2	[12]
TNP-2092	DM8DZKI	Skin and skin-structure infection	1F28-1G0Z	Phase 2	[13]
A-62824	DMJ6IMZ	Discovery agent	N.A.	Investigative	[14]

Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[15]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[16]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[17]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[18]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[17]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[17]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[19]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[17]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[20]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bacterial DNA gyrase (Bact gyrase)	TTN6J5F	GYRA_STAAU; GYRB_STAAU	Inhibitor	[2]
Bacterial DNA topoisomerase 4A (Bact parC)	TTFK8YB	PARC_ECOLI	Inhibitor	[2]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[3]

References

• [1] ClinicalTrials.gov (NCT03696342) Efficacy of the Ophthalmic Pazufloxacin 0.6% for Bacterial Conjunctivitis, Compared to Gatifloxacin 0.3%. (PRO-157). U.S. National Institutes of Health.
• [2] Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.
• [3] Possible involvement of P-glycoprotein in renal excretion of pazufloxacin in rats. Eur J Pharmacol. 2004 Oct 6;501(1-3):151-9.
• [4] Grepafloxacin, a dimethyl derivative of ciprofloxacin, acts preferentially through gyrase in Streptococcus pneumoniae: role of the C-5 group in tar... Antimicrob Agents Chemother. 2002 Feb;46(2):582-5.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] In vitro and in vivo antibacterial activity of T-3912, a novel non-fluorinated topical quinolone. J Antimicrob Chemother. 2002 Mar;49(3):455-65.
• [7] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [8] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [9] Prulifloxacin: a new antibacterial fluoroquinolone. Expert Rev Anti Infect Ther. 2006 Feb;4(1):27-41.
• [10] Dual-targeting properties of the 3-aminopyrrolidyl quinolones, DC-159a and sitafloxacin, against DNA gyrase and topoisomerase IV: contribution to reducing in vitro emergence of quinolone-resistant Streptococcus pneumoniae. J Antimicrob Chemother. 2008 Jul;62(1):98-104.
• [11] Clinical pipeline report, company report or official report of Vyome Therapeutics.
• [12] Antistaphylococcal activities of the new fluoroquinolone JNJ-Q2. Antimicrob Agents Chemother. 2011 Dec;55(12):5512-21.
• [13] Clinical pipeline report, company report or official report of TenNor Therapeutics.
• [14] Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent anti... Bioorg Med Chem Lett. 2006 Mar 1;16(5):1272-6.
• [15] Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
• [16] MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
• [17] Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
• [18] Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
• [19] Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
• [20] Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
• [21] Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.