United States kS^laMIjk Environmental Protection ^J^iniiil m11 Agency EPA/690/R-15/003F Final 9-14-2015 Provisional Peer-Reviewed Toxicity Values for 2-Chlorobenzoic Acid (CASRN 118-91-2) Superfund Health Risk Technical Support Center National Center for Environmental Assessment Office of Research and Development U.S. Environmental Protection Agency Cincinnati, OH 45268 ------- AUTHORS, CONTRIBUTORS, AND REVIEWERS CHEMICAL MANAGER Dan D. Petersen, PhD, DABT National Center for Environmental Assessment, Cincinnati, OH DRAFT DOCUMENT PREPARED BY National Center for Environmental Assessment, Cincinnati, OH This document was externally peer reviewed under contract to Eastern Research Group, Inc. 110 Hartwell Avenue Lexington, MA 02421-3136 Questions regarding the contents of this document may be directed to the U.S. EPA Office of Research and Development's National Center for Environmental Assessment, Superfund Health Risk Technical Support Center (513-569-7300). li 2-Chlorobenzoic Acid ------- TABLE OF CONTENTS COMMONLY USED ABBREVIATIONS AND ACRONYMS iv BACKGROUND 1 DISCLAIMERS 1 QUESTIONS REGARDING PPRTVs 1 INTRODUCTION 2 REVIEW OF POTENTIALLY RELEVANT DATA (NONCANCER AND CANCER) 4 DERIVATION 01 PROVISIONAL VALUES 4 DERIVATION 01 ORAL REFERENCE DOSES 4 Feasibility of Deriving Subchronic and Chronic Provisional Reference Doses (p-RfDs) 4 DERIVATION OF INHALATION REFERENCE CONCENTRATIONS 4 Feasibility of Deriving Subchronic and Chronic Provisional Reference Concentrations (p-RfCs) 4 CANCER WEIGHT-OF-EVIDENCE DESCRIPTOR 4 MODE-OF-ACTION (MOA) DISCI SSION 4 ALTERNATIVE METHODS 5 REFERENCES 6 in 2-Chlorobenzoic Acid ------- COMMONLY USED ABBREVIATIONS AND ACRONYMS a2u-g alpha 2u-globulin MN micronuclei ACGIH American Conference of Governmental MNPCE micronucleated polychromatic Industrial Hygienists erythrocyte AIC Akaike's information criterion MOA mode of action ALD approximate lethal dosage MTD maximum tolerated dose ALT alanine aminotransferase NAG N-acetyl-P-D-glucosaminidase AST aspartate aminotransferase NCEA National Center for Environmental atm atmosphere Assessment ATSDR Agency for Toxic Substances and NCI National Cancer Institute Disease Registry NOAEL no-observed-adverse-effect level BMD benchmark dose NTP National Toxicology Program BMDL benchmark dose lower confidence limit NZW New Zealand White (rabbit breed) BMDS Benchmark Dose Software OCT ornithine carbamoyl transferase BMR benchmark response ORD Office of Research and Development BUN blood urea nitrogen PBPK physiologically based pharmacokinetic BW body weight PCNA proliferating cell nuclear antigen CA chromosomal aberration PND postnatal day CAS Chemical Abstracts Service POD point of departure CASRN Chemical Abstracts Service Registry PODadj duration-adjusted POD Number QSAR quantitative structure-activity CBI covalent binding index relationship CHO Chinese hamster ovary (cell line cells) RBC red blood cell CL confidence limit RDS replicative DNA synthesis CNS central nervous system RfC inhalation reference concentration CPN chronic progressive nephropathy RfD oral reference dose CYP450 cytochrome P450 RGDR regional gas dose ratio DAF dosimetric adjustment factor RNA ribonucleic acid DEN diethylnitrosamine SAR structure activity relationship DMSO dimethylsulfoxide SCE sister chromatid exchange DNA deoxyribonucleic acid SD standard deviation EPA Environmental Protection Agency SDH sorbitol dehydrogenase FDA Food and Drug Administration SE standard error FEVi forced expiratory volume of 1 second SGOT glutamic oxaloacetic transaminase, also GD gestation day known as AST GDH glutamate dehydrogenase SGPT glutamic pyruvic transaminase, also GGT y-glutamyl transferase known as ALT GSH glutathione SSD systemic scleroderma GST glutathione-S-transferase TCA trichloroacetic acid Hb/g-A animal blood-gas partition coefficient TCE trichloroethylene Hb/g-H human blood-gas partition coefficient TWA time-weighted average HEC human equivalent concentration UF uncertainty factor HED human equivalent dose UFa interspecies uncertainty factor i.p. intraperitoneal UFh intraspecies uncertainty factor IRIS Integrated Risk Information System UFS subchronic-to-chronic uncertainty factor IVF in vitro fertilization UFd database uncertainty factor LC50 median lethal concentration U.S. United States of America LD50 median lethal dose WBC white blood cell LOAEL lowest-observed-adverse-effect level iv 2-Chlorobenzoic Acid ------- Final 09-14-2015 PROVISIONAL PEER-REVIEWED TOXICITY VALUES FOR 2-CHLOROBENZOIC ACID (CASRN 118-91-2) BACKGROUND A Provisional Peer-Reviewed Toxicity Value (PPRTV) is defined as a toxicity value derived for use in the Superfund Program. PPRTVs are derived after a review of the relevant scientific literature using established Agency guidance on human health toxicity value derivations. All PPRTV assessments receive internal review by a standing panel of National Center for Environment Assessment (NCEA) scientists and an independent external peer review by three scientific experts. The purpose of this document is to provide support for the hazard and dose-response assessment pertaining to chronic and subchronic exposures to substances of concern, to present the major conclusions reached in the hazard identification and derivation of the PPRTVs, and to characterize the overall confidence in these conclusions and toxicity values. It is not intended to be a comprehensive treatise on the chemical or toxicological nature of this substance. The PPRTV review process provides needed toxicity values in a quick turnaround timeframe while maintaining scientific quality. PPRTV assessments are updated approximately on a 5-year cycle for new data or methodologies that might impact the toxicity values or characterization of potential for adverse human health effects and are revised as appropriate. It is important to utilize the PPRTV database flittp://hhpprtv.ornl.gov) to obtain the current information available. When a final Integrated Risk Information System (IRIS) assessment is made publicly available on the Internet (http://www.epa.eov/iris). the respective PPRTVs are removed from the database. DISCLAIMERS The PPRTV document provides toxicity values and information about the adverse effects of the chemical and the evidence on which the value is based, including the strengths and limitations of the data. All users are advised to review the information provided in this document to ensure that the PPRTV used is appropriate for the types of exposures and circumstances at the site in question and the risk management decision that would be supported by the risk assessment. Other U.S. Environmental Protection Agency (EPA) programs or external parties who may choose to use PPRTVs are advised that Superfund resources will not generally be used to respond to challenges, if any, of PPRTVs used in a context outside of the Superfund program. This document has been reviewed in accordance with U.S. EPA policy and approved for publication. Mention of trade names or commercial products does not constitute endorsement or recommendation for use. QUESTIONS REGARDING PPRTVs Questions regarding the contents and appropriate use of this PPRTV assessment should be directed to the EPA Office of Research and Development's National Center for Environmental Assessment, Superfund Health Risk Technical Support Center (513-569-7300). 1 2-Chlorobenzoic Acid ------- Final 09-14-2015 INTRODUCTION 2-Chlorobenzoic acid (CASRN 118-91-2) is an industrial chemical used as a solvent and an intermediate in the manufacture of surfactants, pharmaceuticals, and other organic compounds. The molecular formula of 2-chlorobenzoic acid (also known as ortho-chlorobenzoic acid) is C7H5CIO2 (see Figure 1). A list of physicochemical properties is provided in Table 1. °^0H /N. XI Figure 1. 2-Chlorobenzoic Acid Structure Table 1. Physicochemical Properties of 2-Chlorobenzoic Acid (CASRN 118-91-2)3 Property (unit) Value Boiling point (°C) 287 Melting point (°C) 140.2 Density (g/cm3 at 20°C) ND Vapor pressure (lmnHg at 25°C) 0.0 pH (unitless) ND Solubility in water (mg/L at 25 °C) 2,090 Relative vapor density (air = 1) ND Molecular weight (g/mol) 156.5675 TliemTDnliis (2015V ND = no data. Table 2 provides a summary of available toxicity values for 2-chlorobenzoic acid from U.S. EPA and other regulatory agencies or organizations. 2 2-Chlorobenzoic Acid ------- Final 09-14-2015 Table 2. Summary of Available Toxicity Values for 2-ChlorobenzoicAcid (CASRN 118-91-2) Sou rce/Parameterab Value (applicability) Reference Noncancer ACGIH NV ACGIH (2015) ATSDR NV ATSDR (2015) Cal/EPA NV Cal/EPA (2014): Cal/EPA (2015a): Cal/EPA (2015b) NIOSH NV NIOSH (2015) OSHA NV OSHA (2011). OSHA (2006) IRIS NV U.S. EPA (2015) DWSHA NV U.S. EPA (2012) HEAST NV U.S. EPA (2011) CARA HEEP NV U.S. EPA (1994) WHO NV WHO (2015) Cancer IRIS NV U.S. EPA (2015) HEAST/WOE NV U.S. EPA (2011) IARC NV IARC (2015) NTP NV NTP (2014) Cal/EPA NV Cal/EPA (2015a): Cal/EPA (2015b): Cal/EPA (2011) "Sources: ACGIH = American Conference of Governmental Industrial Hygienists; ATSDR = Agency for Toxic Substances and Disease Registry; Cal/EPA = California Environmental Protection Agency; CARA = Chemical Assessments and Related Activities; DWSHA = Drinking Water Standards and Health Advisories; HEAST = Health Effects Assessment Summary Tables; HEEP = Health and Environmental Effects Profile; IARC = International Agency for Research on Cancer; IRIS = Integrated Risk Information System; NIOSH = National Institute for Occupational Safety and Health; NTP = National Toxicology Program; OSHA = Occupational Safety and Health Administration; WHO = World Health Organization. ' Parameters: WOE = cancer weight of evidence (U.S. EPA. 20051. NV = not available. Literature searches were conducted on sources published from 1900 through March 2015 for studies relevant to the derivation of provisional toxicity values for 2-chlorobenzoic acid (CASRN 118-91-2). The following databases were searched by chemical name, synonyms, or CASRN: ACGIH, ANEUPL, ATSDR, BIOSIS, Cal/EPA, CCRIS, CDAT, ChemlDplus, CIS, CRISP, DART, EMIC, EPIDEM, ETICBACK, FEDRIP, GENE-TOX, HAPAB, HERO, HMTC, HSDB, IARC, INCHEM IPCS, IP A, ITER, IUCLID, LactMed, NIOSH, NTIS, NTP, OSHA, OPP/RED, PESTAB, PPBIB, PPRTV, PubMed (toxicology subset), RISKLINE, RTECS, TOXLINE, TRI, U.S. EPA IRIS, U.S. EPA HEAST, U.S. EPA HEEP, U.S. EPA OW, and U.S. EPA TSCATS/TSCATS2. The following databases were searched for toxicity values or exposure limits: ACGIH, ATSDR, Cal EPA, U.S. EPA IRIS, U.S. EPA HEAST, U.S. EPA HEEP, U.S. EPA OW, U.S. EPA TSCATS/TSCATS2, NIOSH, NTP, OSHA, and RTECS. 3 2-Chlorobenzoic Acid ------- Final 09-14-2015 REVIEW OF POTENTIALLY RELEVANT DATA (NONCANCER AND CANCER) The available data on 2-chlorobenzoic acid primarily focuses on its biodegradation and biotransformation by microorganisms and its synthesis and use in the development of analytical methods. No information is available regarding repeated-dose oral or inhalation exposure of humans or animals to 2-chlorobenzoic acid. A genetic toxicology study was conducted in Salmonella (Zeiger et at.. 1992). which was negative. The chemical is being tested as part of Tox 21 and is in the NTP 1408 compound library. However, these tests are mechanistic studies and, do not provide endpoints that are currently usable for identifying a point of departure (POD). PubChem lists 263 in vitro assays, in which the only positive result was for antihemorrhagic activity in ddY mouse assessed as inhibition of Protobothrops flavoviridis venom-induced hemorrhagic lesion formation. The only in vivo toxicological data available are median lethal dose (LD50) values in rats of >500 mg/kg oral (NRC. 1953) (Verschueren. 1983). although some references cite this value as being from rabbits, and 2,300 mg/kg intraperitoneally in rabbits (Carminati et at.. 1973). There are also Draize test results in rabbits, where 20 mg was scored moderate in the eye test and 500 mg was scored as mild in the skin test (ChemCas, 2015). There is also some information about metabolism and excretion (Btacktedge et at.. 2000). DERIVATION OF PROVISIONAL VALUES DERIVATION OF ORAL REFERENCE DOSES Feasibility of Deriving Subchronic and Chronic Provisional Reference Doses (p-RfDs) No sub chronic-duration, chronic-duration, developmental toxicity, reproductive toxicity, or carcinogenicity studies on 2-chlorobenzoic acid via the oral route have been identified. Thus, no oral reference doses can be derived. However, as noted below, a computational toxicological surrogate approach was attempted. DERIVATION OF INHALATION REFERENCE CONCENTRATIONS Feasibility of Deriving Subchronic and Chronic Provisional Reference Concentrations (p-RfCs) No sub chronic-duration, chronic-duration, developmental toxicity, reproductive toxicity, or carcinogenicity studies on 2-chlorobenzoic acid via the inhalation route have been identified. Thus, no inhalation reference doses can be derived. However, as noted below, a computational toxicological surrogate approach was attempted. CANCER WEIGHT-OF-EVIDENCE DESCRIPTOR Limitations in the available data preclude development of a weight-of-evidence (WOE) descriptor. MODE-OF-ACTION (MOA) DISCUSSION Limitations in the available data preclude determination of a mode of action (MOA) discussion. 4 2-Chlorobenzoic Acid ------- Final 09-14-2015 ALTERNATIVE METHODS The surrogate approach allows for the use of data from related compounds to calculate screening values when data for the compound of interest are limited or unavailable. Details regarding searches and methods for surrogate analysis are presented in Wane et al. (2012). Three types of potential surrogates (structural, metabolic, and toxicity) are identified to facilitate the final surrogate chemical selection. The surrogate approach may or may not be route-specific or applicable to multiple routes of exposure. All information has been considered together as part of the final WOE approach to select the most suitable surrogate, both toxicologically and chemically. An initial surrogate search focused on identifying structurally similar chemicals with toxicity values from the Integrated Risk Information System (IRIS), PPRTV, and Health Effects Assessment Summary Tables (HEAST) databases to take advantage of the well-characterized chemical-class information. This task was accomplished by searching the U.S. EPA's DSSTox database (DSSTox, 2012) at similarity levels >60% and the National Library of Medicine's ChemlDplus database (ChemlDplus. 2015) at similarity levels >80%. The search revealed several structurally related chemicals could serve as potential surrogates for 2-chlorobenzoic acid. DSS-Tox identified several related chemicals: (1) four dichlorobenzoic acid isomers (2,3-; 2,4-; 2,5-; and 2,6-); (2) two monochlorobenzoic acid isomers (3- and 4-); (3) 2,3,6-trichlorobenzoic acid; and (4) chlorobenzaldehyde. These eight unique compounds had similarity scores over 70%. ChemlDplus identified three others, including 2-iodobenzoic acid, 2-fluorobenzoic acid, and 2-bromobenzoic acid. However, there is no in vivo repeated-dose information on any of these closely related compounds to compare with 2-chlorobenzoic acid for matching health effects. Because 2-chlorobenzoic acid is primarily excreted in the urine as the glycine conjugate (Blackledae et al.. 2000). no other metabolic surrogates are available. The only data available are LD50 values. Due to a lack of repeated-dose toxicity information for any of the potential structural surrogates, derivation of risk values (e.g., oral reference dose [RfD], inhalation reference concentration [RfC], and oral cancer slope factor [OSF]) based on the computational toxicological surrogate approach (Wane et al.. 2012) is not feasible for 2-chlorobenzoic acid. 5 2-Chlorobenzoic Acid ------- Final 09-14-2015 REFERENCES ACGIH (American Conference of Governmental Industrial Hygienists). (2015). 2015 TLVs and BEIs. Based on the documentation of the threshold limit values for chemical substances and physical agents and biological exposure indices [TLV/BEI], Cincinnati, OH. http ://www. aceih.org/forms/store/Product F orm Public/2015-tlvs-and-beis AT SDR (Agency for Toxic Substances and Disease Registry). (2015). Minimal risk levels (MRLs). April 2015. Atlanta, GA: Agency for Toxic Substances and Disease Registry (ATSDR). Retrieved from http://www.atsdr.cdc.gov/mrls/index.asp Biackledge. CA; Partridge. EA; Wilson. ID; Nicholson. JK. (2000). The metabolism and excretion of [14c] 2- and 4-chlorobenzoic acids in the rat. J Pharm Biomed Anal 22: 1023-1028. http://dx.doi.org/10.1016/S0731-7085(00)00295-8 Cal/EPA (California Environmental Protection Agency). (201 1). Hot spots unit risk and cancer potency values. Appendix A. Sacramento, CA: Office of Environmental Health Hazard Assessment, http://www.oehha.ca.gov/air/hot spots/2009/AppendixA.pdf Cal/EPA (California Environmental Protection Agency). (2014). All OEHHA acute, 8-hour and chronic reference exposure levels (chRELs) as of June 2014. Sacramento, CA: Office of Health Hazard Assessment, http://www.oehha.ca.gov/air/allrels.html Cal/EPA (California Environmental Protection Agency). (2015a). Chemicals known to the state to cause cancer or reproductive toxicity August 25, 2015. (Proposition 65 list). Sacramento, CA: California Environmental Protection Agency, Office of Environmental Health Hazard Assessment. http://oehha.ca.gov/prop65/prop65 list/files/P65single060614.pdf Cal/EPA (California Environmental Protection Agency). (2015b). OEHHA toxicity criteria database [Database], Sacramento, CA: Office of Environmental Health Hazard Assessment. Retrieved from http://www.oehha.ca.gov/tcdb/index.asp Carminati- GM; Chiabotto. L; Duzzi. L. (1973). [Inhibition of the appearance of gastric ulcers in rats, using benzoic acid derrivatives]. Boll Chim Farm 112: 53-63. ChemCas. (2015). Chemical information net [Database]: Leputech HPLC Laboratory. Retrieved from http://chemcas.org/ ChemlDplus. (2015). ChemlDplus - a TOXNET database. Bethesda, MD: National Institutes of Health, U.S. Library of Medicine. Retrieved from http: //chern. si s. nlm. nih. gov/chemi dptus/ DSSTox (Distributed Structure-Searchable Toxicity). (2012). DSSTox database [Database], Research Triangle Park, NC: U.S. Environmental Protection Agency, National Center for Computational Toxicology. Retrieved from http://www.epa.gov/ncct/dsstox/ IARC (International Agency for Research on Cancer). (2015). I ARC Monographs on the evaluation of carcinogenic risk to humans. Geneva, Switzerland: International Agency for Research on Cancer, WHO. http://monographs.iarc.fr/ENG/Monographs/PDFs/index.php NIOSH (National Institute for Occupational Safety and Health). (2015). N10SH pocket guide to chemical hazards. Index of chemical abstracts service registry numbers (CAS No.). Atlanta, GA: Center for Disease Control and Prevention, U.S. Department of Health, Education and Welfare, http://www.cdc.gov/niosh/npg/npgdcas.html NRC (National Research Council). (1953). Chemical-biological coordination center, review. Washington, DC: National Academies of Science. 6 2-Chlorobenzoic Acid ------- Final 09-14-2015 NTP (National Toxicology Program). (2014). Report on carcinogens. Thirteenth edition. Research Triangle Park, NC: U.S. Department of Health and Human Services, Public Health Service, http://ntp.niehs.nih.eov/pubhealth/roc/rocl3/index.html OSHA (Occupational Safety & Health Administration). (2006). Table Z-l limits for air contaminants. Occupational safety and health standards, subpart Z, toxic and hazardous substances. (OSHA standard 1910.1000). Washington, DC: U.S. Department of Labor. http://www.osha.gov/pls/oshaweb/owadisp.show document?p tabte=STANDARDS&p id=9992 OSHA (Occupational Safety & Health Administration). (201 1). Air contaminants: occupational safety and health standards for shipyard employment, subpart Z, toxic and hazardous substances. (OSHA Standard 1915.1000). Washington, DC: U.S. Department of Labor. http://www.osha.gov/pls/oshaweb/owadisp.show document?p tabte=STANDARDS&p id=10286 U.S. EPA (U.S. Environmental Protection Agency). (1994). Chemical assessments and related activities (CARA) [EPA Report], (600/R-94/904; OHEA-I-127). Washington, DC: U.S. Environmental Protection Agency, Office of Health and Environmental Assessment. http://nepis.epa. gov/Exe/ZyPURL.cgi?Dockev=6000 lG8L.txt U.S. EPA (U.S. Environmental Protection Agency). (2005). Guidelines for carcinogen risk assessment. (EPA/630/P-03/001F). Washington, DC: U.S. Environmental Protection Agency, Risk Assessment Forum, http://www.epa.gov/cancerguidelines/ U.S. EPA (U.S. Environmental Protection Agency). (201 1). Health effects assessment summary tables (HEAST). Washington, DC: U.S. Environmental Protection Agency, Office of Emergency and Remedial Response, http://epa-h.east.ornl.gov/ U.S. EPA (U.S. Environmental Protection Agency). (2012). 2012 Edition of the drinking water standards and health advisories [EPA Report], (EPA/822/S-12/001). Washington, DC: Office of Water. http://water.epa.gov/action/advisories/drinking/upload/dwstandards2012.pdf U.S. EPA (U.S. Environmental Protection Agency). (2015). Integrated risk information system (IRIS) [Database], Washington, DC: U.S. Environmental Protection Agency, Integrated Risk Information System. Retrieved from http://www.epa.gov/iris/ Verschueren. K. (1983). Handbook of environmental data on organic chemicals (2nd ed ed.). New York, NY: Van Nostrand Reinhold Company. Wang. ( NY: Zhao. QJ; Wesselkamper. SC; Lambert. JC; Peterson. D; Hess-Wilson. JK. (2012). Application of computational toxicological tools and approaches in human health risk assessment. I. A tiered surrogate approach. Regul Toxicol Pharmacol 63: 10-19. WHO (World Health Organization). (2015). Online catalog for the Environmental Health Criteria (EHC) monographs. Geneva, Switzerland: World Health Organization (WHO). http://www.who.int/ipcs/publications/ehc/en/ Zeiger. E; Anderson. B; Haworth. S; Law!or. T; Mortelmans. K. (1992). Salmonella mutagenicity tests: V Results from the testing of 311 chemicals. Environ Mol Mutagen 19: 2-141. http://dx.doi.org/10.1002/em.28501906Q3 7 2-Chlorobenzoic Acid ------- |